1. Kinase Inhibitors - wako
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1. Kinase Inhibitors - wako
1. Kinase Inhibitors Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition 909910-43-6 DMSO - Keep at -20℃. Summary A-83-01 【TGF-β R I Kinase Inhibitor IV】 018-22521 2 mg 014-22523 10 mg for Cellbiology 1. Kinase Inhibitors Product Name <Protein kinase inhibitor> Selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7. Inhibits Smad2/3 phosphorylation and TGF-β-induced epithelial-to-mesenchymal transition. This product has little or no effect on bone morphogenetic protein type I receptors, p38 MAP kinases, and extracellular-regulated kinases. 17-AAG, 97.0+ % (HPLC) 012-20101 1 mg for Cellbiology 75747-14-7 DMSO, methanol EC50 of HSP90 = 7.2 μM Keep at -20℃. <Protein kinase inhibitor/ protein tyrosine kinase (PTK) inhibitor> Synthetic derivative of geldanamycin, which is one of the ansamycin antibiotics. 17-AAG inhibits the function of HSP90 by binding to the ATP binding site of HSP90. HSP90 inhibitors dephosphorylate Akt resulting in inactivation of Akt and apoptosis. AG 490, 95+% (TLC) 013-17181 5 mg for Biochemistry 134036-52-5 DMSO, DMF, methanol IC50 of Dephosphorylation of EGF receptor tyrosine kinase: 1.2 μmol; EGF dependent cell proliferation: 6 μmol Keep at -20℃. <PTK inhibitor> Specific and potent JAK-2 protein tyrosine kinase inhibitor. Also inhibits EGF receptor autophosphorylation. AG 1296 016-20121 5 mg for Cellbiology 146535-11-7 DMSO - Keep at -20℃. <PTK inhibitor> It inhibits signaling in human PDGF (platelet-derived growth factor) α receptor, PDGF β receptor, stem cell stimulating factor c-kit and FGF (fibroblast growth factor) receptor. AG 1478 017-20151 5 mg for Cellbiology 175178-82-2 DMSO - Keep at -20℃. <PTK inhibitor> Potent and selective inhibitor of EGF receptor kinase. Decrease in EGF-stimulating DNA synthesis and inhibition of activation of EGFdependent src family kinase have been reported. ALK5 Inhibitor, 96.0+ % (HPLC) 012-23021 1 mg for Cellbiology 446859-33-2 methanol - Keep at -20℃. <Protein kinase inhibitor> Potent and selective ATP-competitive inhibitor of TGF-β RI kinase/ALK5. Can be used as substitute of Sox2 or c-Myc (Yamanaka 4 factors) in induction of murine iPS cells. Aminogenistein, 90.0+ % (HPLC) 017-15901 1 mg for Biochemistry 132018-32-7 Ethanol, DMSO IC50 of lck = 1.2 μM Keep at -20℃. <PTK inhibitor> Inhibitor of PTK, especially p56lck. The product, even among other flavons, is able to specifically inhibit lck activity at a low dose and is therefore employed as an useful tool for clarification of the mechanism of immune response activation. Apigenin, 95+ % (TLC) 010-18914 5 mg 016-18911 10 mg 012-18913 50 mg for Biochemistry 520-36-5 Methanol - Keep at 2-10℃. <MAP kinase inhibitor> Plant flavonoid. It changes phenotypes of many ras transformed cells to the original form. This is achieved by inhibition of signal transduction route mediating MAP (Miogen Activated Protein) kinase (MAPK). In case of NIH3T3 cells transformed by v-H-ras, treatment with apigenin (12.5 μM) induces dephosphorylation of p44 MAPK resulting in a decrease in MAP kinase activity. AS 604850, 98.0+ % (HPLC) 015-23131 5 mg for Cellbiology 648449-76-7 DMSO IC50 of PI3Kα: 4.5 μM; PI3Kγ: 250 nM; PI3Kβ, PI3Kδ: 250 nM Keep at 2 - 10℃ <Protein kinase inhibitor> Thiazolidine-dione compound, which is a potent, cell permeable and ATP-competitive inhibitor of PI3K γ. It exhibits highly selectivity. 1 1. Kinase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in 648450-29-7 DMSO IC50 Storage Condition Summary AS 605240, 95.0+ % (HPLC) 012-23141 5 mg for Cellbiology IC50 of PI3Kα: 60 nM; PI3Kγ: 270 nM; PI3Kβ: 8 nM; PI3Kδ: 300 nM Keep at 2 - 10℃ <Protein kinase inhibitor> Thiazolidine-dione compound, which is a potent, cell permeable and ATP-competitive inhibitor of PI3K γ (Ki = 180 nM). It exhibits highly selectivity. ATM Kinase Inhibitor, 97.0+ % (HPLC) 015-22911 2 mg for Cellbiology 587871-26-9 Ethanol ATM: IC50 = 13 nM; Ki = 2.2 nM Keep at -20℃. <Cyclin-Dependent Kinase (CDK) Inhibitor> Cell-permeable, ATP-competitive inhibitor of ATM kinase. Shows high ATM kinase selectivity for PIKK and PI3K family kinases. 6-Bromoindirubin-3'-oxime【BIO】 【GSK-3 Inhibitor IX】, 95.0+ % (HPLC) 029-16241 1 mg for Cellbiology 667463-62-9 - - Keep at 2 - 10℃ <Protein kinase inhibitor> Potent and reversible ATP-competitive inhibitor. It shows to activate the Wnt signaling pathway and maintain pluripotencies in human and murine ES cells and also promotes cardiomyocyte proliferation and acts as a GSK-3 inhibitor. Butein, 98.0+ % (HPLC) 027-14461 10 mg for Biochemistry 487-52-5 Methanol, DMSO - Keep at -20℃. <Protein tyrosine kinase (PTK) inhibitor> Tyrosine kinase inhibitor isolated from plant polyphenols. Reported to activate SIrt1 (Class III HDAC). Calphostin C, 95.0+ % (HPLC) 030-15133 50 μg 034-15131 100 μg for Cellbiology 121263-19-2 DMSO, DMF IC50 of PKC: 50 nM; HeLa S3: 0.23 μg/mL; MCF-7: 0.18 μg/mL Keep at 2-10℃. <Protein kinase C (PKC) inhibitor> Specific protein kinase C (PKC) inhibitor. Shows strong anticellular activity against a variety of cultured cells. Carbonyl Cyanide m-Chlorophenylhydrazone, 97+% (TLC) 034-16993 100 mg 038-16991 1g for Biochemistry 99534-03-9 Ethanol, acetone - Keep at -20℃. - Keep at -20℃. <Protein kinase inhibitor> Potent uncoupler of oxidative phosphorylation that inhibits mitochondrial function. CKI-7 Dihydrochloride, 97.0+ % (HPLC) 034-21501 5 mg for Cellbiology - Water <Protein kinase inhibitor> Casein kinase (CK1) inhibitor. Use with SB431542 and Y-27632 induces differentiation of human ES cells and human iPS cells into retinal progenitor cells in serum- and feeder cell-free culture medium. Compound 15e, 98.0+ % (HPLC) 031-21491 5 mg for Cellbiology 371943-05-4 Ethanol IC50 of PI3Kα: 2 nM; PI3Kβ: 16 nM; PI3Kγ: 660 nM; PI3KC2β: 220 nM Keep at 2 - 10℃ <Protein kinase inhibitor> Permeable morpholino pyrimidine compound. A highly selective PI3Kα inhibitor. Compound 401, 98.0+ % (HPLC) 033-21951 1 mg 039-21953 5 mg for Cellbiology 168425-64-7 Methanol IC50 of DNA-PK: 0.28 μM; mTOR: 5.3 μM; ATM, ATR > 100 μM Keep at -20℃. <Protein kinase inhibitor> Reversible and selective DNA-PK and mTOR inhibitor. It exhibits negligible affinity to PI3K, ATM and ATR. It has been known to inhibit mTORdependent proliferation and induce apoptosis in TSC1-/- mouse embryo fibroblasts. Deguelin 047-29211 5 mg for Cellbiology 522-17-8 Acetone, dichloromethane, acetonitrile, DMSO - Keep at 2-10℃. <Akt inhibitor> Akt (Protein Kinase B; PKB) inhibitor. It inhibits proliferation of cells in the GM-2 stage of cell cycle. It induces apoptosis in the precancerous and cancerated cell lines. 2 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name CAS No. Grade Soluble in IC50 Storage Condition Water, glacial acetic acid, ethanol, acetone and chloroform. - Keep at RT. - Keep at 2 - 10℃ Summary Dibucaine Hydrochloride, 98.0+ % (after drying)(Titration) 049-20011 1g for Biochemistry 61-12-1 1. Kinase Inhibitors Wako Cat. No. Pkg. Size <Protein kinase inhibitor> Lipophilic PKC inhibitor. Inhibits Na+ and K+-ATPase activities, too. Dorsomorphin, 99.6% (HPLC, the initiall lot) 045-31221 1 mg 041-31223 5 mg for Cellbiology 866405-64-3 Methanol <Protein kinase inhibitor> Permeable pyrazolopyrimidine compound, which is potent, selective and reversible ATP-competitive inhibitor of AMPK (AMP-activated protein kinasse). It has been shown to inhibit BMP signal strongly by inhibition of BMP type I receptors (ALK-2, ALK-3 and ALK- 6). Dorsomorphin Dihydrochloride, 98.0+ % (HPLC) 047-31801 1 mg 043-31803 5 mg for Cellbiology 1219168-18-9 Water - Keep at 2 - 10℃ <Protein kinase inhibitor> This substance inhibits bone morphogenic factor (BMP) type I receptors (ALK2, ALK3 and ALK6). It has been shown to inhibit BMP signal necessary for embryogenesis and accelerates important nerve differentiation from human pluripotential stem cells. It also functions as a potent, selective and reversible ATP-competitive inhibitor of AMP-activating protein kinase (AMP-K). Geldanamycin, from Streptomyces hygroscopicus, 95.0+ % (HPLC) 077-04571 100 μg for Biochemistry 30562-34-6 Methanol Keep at -20℃. - <Protein kinase inhibitor> This product is an antitumor agent that has a benzoquinoid skeleton and has a pp60src tyrosine kynase inhibitory potency. Its pharmacological action is more potent than that of herbimycin, which has a similar structure. Genistein, 98.0+ % (HPLC) 073-05531 20 mg 079-05533 100 mg for Cellbiology 446-72-0 Ethanol - Keep at -20℃. <Protein tyrosine kinase (PTK) inhibitor> Isoflavone compound. Tyrosine kinase inhibitor by antagonizing against ATP. Known to inhibit the proliferation of various solid tumor cells and induce the differentiation of the tumor cells. Genistin, from Soybean; 98.0+ % (HPLC) 070-04681 10 mg 076-04683 100 mg for Biochemistry 529-59-9 Hot methanol - Keep at 2-10℃. <Protein tyrosine kinase (PTK) inhibitor> Soy extract isoflavone, or glucoside. Cancer-suppressing effects, antioxidant effects, and osteoporosis preventive effects have been reported. GF 109203X, 90.0+ % (HPLC) 079-03811 1 mg for Cellbiology 133052-90-1 DMSO IC50 of PKC: 10 nM Keep at 2 - 10℃ <Protein kinase inhibitor / protein kinase C (PKC) inhibitor> Potent and selective PKC inhibitor among bisindolylmaleimides, which have an inhibatory action on PKC. The structure is similar to that of staurosporine. Gö 6983 070-05801 1 mg for Cellbiology 133053-19-7 DMSO IC50 of PKCα: 7 nM; PKCβ: 7 nM; PKCγ: 6 nM; PKCδ: 10 nM; PKCζ: 60 nM; PKCμ: 20μM Keep at -20℃. <Protein kinase C (PKC) inhibitor> Cell-permeable PKC inhibitor GSK 269962A, 97.0+ % (HPLC) 070-05921 2 mg for Cellbiology 850664-21-0 DMSO, acetonitrile IC50 of ROCK-I: 1.6 nM; ROCK-II: 6 nM Keep at 2 - 10℃ <Protein kinase inhibitor> ROCK Inhibitor. Not available for sale in the USA due to patent. 3 1. Kinase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in 850664-21-0 Ethanol, DMSO, water IC50 Storage Condition Summary GSK 429286A, 97.0+ % (HPLC) 073-05911 2 mg for Cellbiology IC50 of ROCK: 14 nM Keep at 2 - 10℃ <Protein kinase inhibitor> ROCK inhibitor. It cancels out adrenaline-induced contraction of the aortic valve in rats and lowers the mean blood pressure in the arteries of hypertensive rats. H-1152 Dihydrochloride 088-09281 1 mg for Cellbiology 871543-07-6 Water IC50 of ROCK-II: 12 nM Keep at -20℃. <Protein kinase inhibitor> ROCK inhibitor. Its inhibitory activity is more potent than that of Y-27632. It exhibits weak affinity to other serine/threonine kinases. Herbimycin A, 98.0+ % (HPLC) 085-06491 1 mg for Biochemistry 70563-58-5 Methanol, DMSO - Keep at 2-10℃. <Protein tyrosine kinase (PTK) inhibitor> Tyrosine kinase inhibitor by binding to the SH group of cysteine in oncogene src. It also inhibits transformation activity of oncogenes (src, yes, fps, ros, abl, erbB) that have tyrosine kinase activity. It also has the unique ability to restore RSVts-NRK cells to their normal form. Hypericin, from Hypericum perforatum 086-07761 1 mg 082-07763 5 mg for Biochemistry 548-04-9 Water-THF - Keep at 2 - 10℃ <Protein kinase inhibitor / PKC inhibitor> Inhibitor of PKC, insulin receptor, EGF receptor, casein kinase II, and thyrosine kinase activity of MAPK. It also exhibits antivirus and antiretrovirus activities. IPA-3, 97.0+ % (HPLC) 093-06231 5 mg for Cellbiology 42521-82-4 DMSO, acetonitrile PAK1: IC50 = 2.5 μM Keep at 2 - 10℃ <Protein kinase inhibitor> p21 activation kinase (PAK) inhibitor, which binds to the regulatory domain of PAK and accelerates inactivation of PAKs structure. Shows high selectivity to PAK1 in particular. PAK1 involves in tumor formation and metastasis. K-252a 113-00561 50 μg 119-00563 100 μg 117-00564 250 μg for Biochemistry 97161-97-2 Ethyl acetate - Keep at -20℃. <Protein kinase inhibitor / PKC inhibitor> Selective inhibitor of PKA (cyclic AMP-dependent protein kinase), PKC (phospholipid-dependent protein kinase) and PKG (cyclic GMPdependent protein kinase). K-252b 110-00571 50 μg 114-00574 250 μg for Biochemistry 99570-78-2 Methanol - Keep at -20℃. <Protein kinase inhibitor / PKC inhibitor> Selective inhibitor of PKA (cyclic AMP-dependent protein kinase), PKC (phospholipid-dependent protein kinase) and PKG (cyclic GMPdependent protein kinase). Kenpaullone 110-00831 1 mg 116-00833 5 mg for Cellbiology 142273-20-9 DMSO - Keep at -20℃. <CDK Inhibitor> Potent GSK-3β and CDK inhibitor. Inhibits antagonistically ATP binding. Reported to be substitutable for Klf4, one of the 4 Yamanaka factors (Oct3/4, Klf4, Sox2, c-Myc), in iPS cell production. Also reported to improve reprogramming efficiency if added upon the introduction of 4 Yamanaka factors. Ki 8751, 96.0+ % (HPLC) 112-00891 5 mg for Cellbiology 228559-41-9 DMSO IC50 = 0.9 nM Keep at -20℃. <Protein kinase inhibitor> Potent and selective VEGFR-2 tyrosine kinase inhibito. 4 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Grade CAS No. Soluble in for Biochemistry 127191-97-3 Methanol, DMSO IC50 Storage Condition Summary KN-62 118-00631 1 mg 114-00633 5 mg Ca2+ / calmodulin-dependent protein kinase II (in rat brain): IC50 = 0.3 μM Keep at 2-10℃. 1. Kinase Inhibitors Wako Cat. No. Pkg. Size <Kinase inhibitor / Calmodulin antagonist> Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. It inhibits the proliferation of K562 cells (1 μM). KN-93 115-00641 1 mg 111-00643 5 mg for Biochemistry 139298-40-1 Methanol Ca2+ / calmodulin-dependent protein kinase II (in rat brain): IC50 = 2.0 μM Keep at 2-10℃. <PKC inhibitor / Calmodulin antagonist> Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. Inhibits insulin release from isolated islands of Langerhans caused by glucose induction and forskolin stimulation. It induces stoppage of the cell cycle in theG1 phase and apoptosis in NIH3T3 cells. KN-93, Water-Soluble 114-00731 1 mg for Cellbiology - Water - Keep at -20℃. <PKC inhibitor> Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. Inhibits insulin release from isolated islands of Langerhans caused by glucose induction and forskolin stimulation. It induces stoppage of the cell cycle in theG1 phase and apoptosis in NIH3T3 cells. KT 5720 117-00581 50 μg 113-00583 100 μg 111-00584 250 μg for Biochemistry 108068-98-0 Methanol - Keep at -20℃. - Keep at -20℃. <Protein kinase inhibitor> K252a derivative and membrane permeable PKA (cyclic AMP-dependent protein kinase) inhibitor KT 5823 114-00591 50 μg 110-00593 100 μg 118-00594 250 μg for Biochemistry 126643-37-6 Ethyl acetate, methanol <PKC inhibitor> Cell-permeable PKC inhibitor KU 0063794, 98.0+ % (HPLC) 115-00881 5 mg for Cellbiology 938440-64-3 Acetone, dichloromethane, IC50 of mTOR1: 10 nM; mTOR2: 10 nM. acetonitrile, DMSO Keep at 2-10℃. <Akt inhibitor> Selective mTOR (mammalian target of rapamycin) inhibitor. Shows no inhibitory activity against 76 types of protein kinases including PI3K even at 1,000-fold concentration. LDN 193189 Hydrochloride, 98.0+ % (HPLC) 124-06011 2 mg for Cellbiology 1062368-62-0 Water IC50 of ALK2: 5 nM; ALK3: 30 nM. Keep at 2 - 10℃ <Protein kinase inhibitor> This product inhibits ALK2 and ALK3, which are BMP type I receptors, and consequently inhibits phosphorylation of Smad1, Smad5 and Smad8. LY 294002, 97.0+%(HPLC) 129-04861 5 mg 125-04863 10 mg 123-04864 25 mg for Biochemistry 154447-36-6 Ethanol, acetone IC50 of PI3-kinase: 1.4 μM; Histamine secretion by PBL-2H3: 5 μM. Keep at 2-10℃. <Akt inhibitor> Highly cell-permeable, specific phosphatidylinositol 3-kinase (PI3-kinase) inhibitor. It inhibits the proliferation of rabbit aorta smooth muscle cells without inducing apoptosis. It is also reported to inhibit histamine secretion by RBL-2H3 cells. 5 1. Kinase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade/Manufacturer CAS No. Soluble in IC50 Storage Condition Summary Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-Ala-Phe-Asp-Ala-Tyr 331-43741 0.5 mg Peptide Institute (4374-v) - Water 5142-23-4 - Keep at -20℃. IC50 = 4.1 nM <Protein kinase inhibitor> Inhibitor of calmodulin-dependent protein kinase II. 3-Methyladenine 131-17671 100 mg 137-17673 1g for Biochemistry - Keep at -20℃. <PI3 kinase inhibitor> This product prevents downstream mTOR kinase activity degradation by inhibition of PI3-kinase , which in turn suppresses autophagy. NSC 693868, 98.0+ % (HPLC) 140-08891 5 mg for Cellbiology 40254-90-8 DMSO - Keep at 2 - 10℃ 154447-35-5 DMSO IC50 of DNA-PK: 0.23 μM; PI3K: 13.0 μM; ATM, ATR >100 μM Keep at 2 - 10℃ <Protein kinase inhibitor> Selective inhibitor of GSK-3β and CDK5. NU 7026, 97.0+ % 145-08841 5 mg for Cellbiology <Protein kinase inhibitor> ATP-competitive inhibitor of the protein kinase DNA-PK (DNA-dependent protein kinase). NU 7441, 98.0+ % (HPLC) 143-09001 1 mg 149-09003 5 mg for Cellbiology 503468-95-9 Methanol IC50 of DNA-PK: 14 μM; mTOR: 1.7 μM; PI3K: 13.0 μM; ATM, ATR >100 μM Keep at -20℃. <Protein kinase inhibitor> Potent, reversible and selective inhibitor of DNA-PK (DNA-dependent protein kinase) and mTOR. Has little affinity with PI3K, ATM, and ATR. Known to inhibit mTOR-dependent proliferation and induce apoptosis in TSC1-/- mouse embryonic fibroblasts. Olomoucine, 97+ % (TLC) 157-01901 5 mg for Biochemistry 101622-51-9 DMSO - Keep at -20℃. <CDK Inhibitor / MAPK inhibitor> It inhibits p34cdc/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, cerebral p33cdk5/p35 and erk1/MAPK, and it has been reported to inhibit in vitro the transition of the G2/M phase in the oocytes of starfish, and the transition of the G1/S phase in the mesophyll protoplasts of petunia. PD-98059, 95+ % (TLC) 169-19211 5 mg for Biochemistry 167869-21-8 Ethanol, acetone - Keep at -20℃. <Protein kinase inhibitor/ MAPK inhibitor> MAPK-1 inhibitor. This product has been reported to inhibit MAPK activation by insulin and block completely the increase in cell growth and MAP activity induced by leptin (obesity regulating hormone). The resting cell pretreated with PD-98059 has been demonstrated to inhibit a great deal the expression of the advance early genes c-fos and eggr-1 induced by a peroxisome proliferative agent. PD 173074 166-24351 5 mg for Cellbiology 219580-11-7 Methanol - Keep at 2-10℃. <PTK inhibitor> ATP competitive type FGF receptor inhibitor. The FGF signaling pathway is associated with spontaneous proliferation of stem cells in a host of systems. PD 184352, 98.0+ % (HPLC) 169-25181 5 mg for Cellbiology 212631-79-3 Methanol, DMSO - Keep at 2-10℃. <MAPK Inhibitor> Poteent and selective inhibitor of MEK1. Recent studies showed that culturing ES cells in a medium containing CHIR99021, SU5402, PD184352 allows for highly-efficient suppression of differentiation. 6 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Grade CAS No. Soluble in for Cellbiology 391210-10-9 Methanol, DMSO IC50 Storage Condition Summary PD 0325901 162-25291 5 mg 168-25293 25 mg IC50 of MEK: 0.33 nM Keep at -20℃. 1. Kinase Inhibitors Wako Cat. No. Pkg. Size <MAPK Inhibitor> MAPK inhibitor with potent antitumor activity. It induces phosphorylation of MAPK, inhibition of its activation and inhibition of tumor cell proliferation. PD0325901 inhibits MAPK activity without adverse reactions. Addition of this product and CHIR99021 to a culture medium results in efficient culture of mouse ES cells. Phloretin, 98.0+ % (HPLC) 160-17781 250 mg for Biochemistry 60-82-2 Methanol IC50 = 16 μM Keep at 2 - 10℃ <PKC inhibitor> The aglycone moiety of phlorizin, a specific inhibitor of the sugar active transport system, which is actually responsible for the inhibitory action of phlorizin. When used alone, phloretin has been reported to be less effective for the active transport system while it is known to be more inhibitory than phlorizin to the carrier transport system, suggesting a difference in the mode of action according to structure. It is also useful as means for the study of the kinetics and regulatory mechanisms of PKC as a non-specific inhibitor of PKC. PI-103, 98.0+ % (HPLC) 163-24241 1 mg 169-24243 10 mg for Cellbiology 371935-74-9 DMSO - Keep at -20℃. <Akt inhibitor> Potent, cell-permeable and ATP-competitive inhibitor of DNA-PK, PI-3K, and mTOR with selectivity for a wide range of lipids and protein kinases. Reported to inhibit PIP3 production, insulin signal transduction, and Akt phosphorylation, suppress cell proliferation, and induce cell death. Piceatannol 169-21661 10 mg for Cellbiology 10083-24-6 Ethanol - Keep at 2 - 10℃ <Protein kinase inhibitor / PTK inhibitor> Selective inhibitor of non-reception type tyrosine kinase Syk. An activator of human deacetylase class III (SIrt1). PIK-75 Hydrochloride, 98.0+ % (HPLC) 162-24451 5 mg for Cellbiology - Water-methanol IC50 of PI3Kα: 0.3 nM; PI3Kβ: 850 nM; PI3Kγ: 40 nM; PI3K C2β: 100 nM Keep at 2 - 10℃ <Protein kinase inhibitor> Cell-permeable imidazopyridine compound, which is a selective inhibitor of PI3Kα. PKC 412, 96.0+ % (HPLC) 164-25751 1 mg 160-25753 10 mg for Cellbiology 120685-11-2 - - Keep at -20℃. <Protein kinase inhibitor> Wide range of kinase inhibitor. Inhibits PKC, PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1,EGFR, etc. PP 2, 94.0+ % (HPLC) 166-20331 1 mg for Biochemistry 172889-27-9 Methanol, DMSO - Keep at -20℃. 5334-30-5 Methanol - Keep at -20℃. 1092351-67-1 DMSO IC50 of mTOR: 8 nM; PI3Kα: 2 μM; PI3Kβ: 2.2 μM; PI3Kγ: 1.3 μM; PI3Kδ: 0.1 μM Keep at 2-10℃. <PTK inhibitor> Src family tyrosine kinase inhibitor. PP 3, 94.0+ % (HPLC) 163-20341 1 mg for Biochemistry <PTK inhibitor> EGF receptor type tyrosine kinase inhibitor PP 242, 98.0+ % (HPLC) 165-24441 5 mg for Cellbiology <Akt inhibitor> Potent and selective mTOR (mammalian target of rapamycin) inhibitor 7 1. Kinase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Practical Grade 6151-25-3 Ethanol, acetone - Keep at RT. Summary Quercetin Dihydrate 171-00404 100 mg 177-00401 1g 173-00403 10 g <Akt inhibitor> Yellow flavonoid. Has antioxidant and anti-tumor effects. Its fat absorption inhibitory effect is particularly strong compared with other polyphenols, and it aids in eliminating the body fat. Boosts the fat metabolism in the liver, increases fat combustion, and inhibits fat absorption by binding to fat in the digestive tract. Also said to reduce the inflammation in pollinosis. Rac1 Inhibitor, 98.0+ % (HPLC) 180-02491 5 mg for Cellbiology - Water - Keep at 2-10℃. <MAPK Inhibitor> Selective inhibitor of Rac1-GEF interaction. Specifically inhibits Rac1 activity by inhibiting the interactions between Rac1 and Rac-specific GEFs (guanine nucleotide exchange factors), TrioN and Tiam1. Radicicol, 97.0+ % (HPLC) 183-01901 1 mg for Cellbiology 12772-57-5 Ethanol, methanol, DMSO - Keep at -20℃. <PTK inhibitor> Macrocyclic lactone antifungal antibiotic with antimalarial activity. It inhibits a heat shock protein 90 (HSP90) and protein tyrosine kinase. Rapamycin (mixture of isomers) 184-02531 1 mg 180-02533 10 mg 188-02534 50 mg for Cellbiology 53123-88-9 - - Keep at -20℃. <Protein kinase inhibitor> Macrolide immunosuppressive agent. A structural analog of FK506 that binds to FK506 binding proteins (FKBPs) but does not inhibit calcineurin activity. The rapamycin-FKBP complex inhibits the signal from IL-2 by inhibiting the kinase activity of mTOR. Inhibits G1-to-S phase transition of the cell cycle. RG-14620 188-02811 10 mg 184-02813 50 mg for Cellbiology 136831-49-7 - 138489-18-6 Ethanol IC50 = 3μM Keep at -20℃. IC50 of PKCα: 5 nM; PKCβI: 24 nM; PKCβII: 14 nM; PKCγ: 27 nM; PKCε: 24 nM; PKA: 0.9 μM; CaM kinase II: 17 μM Keep at 2-10℃. <Protein kinase inhibitor> EGFR tyrosine kinase inhibitor Ro 31-8220 Methanesulfonate 186-02591 1 mg for Cellbiology <PKC inhibitor> A structural analog of staurosporine. Potent, cell-permeable PKC inhibitor. Its selectivity for PKAs and CaM kinase II is low, and it also has inhibiting effects on glycogen synthase kinase 3 (GSK3) and voltage-dependent Na channels. Roscovitine, 98.0+ % (HPLC) 182-01591 1 mg 188-01593 10 mg for Biochemistry 186692-46-6 DMSO, ethanol, acetone - Keep at -20℃. <CDK inhibitor> Olomoucine analog and CDK2 and CDK5 inhibitor. In Alzheimer's disease, it is believed to be associated with hyperphosphorylated tau. SB 202190 193-13531 1 mg for Cellbiology 152121-30-7 Methanol - Keep at -20℃. <MAPK Inhibitor> Potent and selective inhibitor of the p38α and β isoforms of p38 MAPK family. Shows membrane permeability. It has no effect on ERK and JNK MAPK. 8 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Grade CAS No. Soluble in 152121-47-6 DMSO, methanol IC50 Storage Condition Summary SB 203580, 98.0+ % (HPLC) 199-16551 1 mg 195-16553 10 mg for Cellbiology IC50 of SAPK2a / p38: 50 nM; SAPK2b / p38β2: 50 nM Keep at -20℃. 1. Kinase Inhibitors Wako Cat. No. Pkg. Size <Protein kinase inhibitor / MAPK inhibitor> Specific MAPK p38α and p38β inhibitor. Also used to separate and maintain embryonic stem cells (ES cells). SB 203580 Hydrochloride, 98.0+ % (HPLC) 198-16761 1 mg for Cellbiology 869185-85-3 Water IC50 of p38α (in vitro): 34 nM; (in vivo): 600 nM Keep at -20℃. <MAPK Inhibitor> Specific MAPK p38α and p38β inhibitor. Also used to separate and maintain embryonic stem cells (ES cells). SB 415286, 98.0+ % (HPLC) 197-15751 5 mg for Cellbiology 264218-23-7 DMSO - Keep at -20℃. <Protein kinase inhibitor> Potent, cell-permeable, and selective GSK-3 inhibitor. GSK-3β inhibitors are used in a variety of stem cell research including ES cells and iPS cells. Reduces the cell death of cerebellar granule neurons in vivo. Also increases cytoplasmic β-catenin concentration and inhibits GSK-3-dependent tau phosphorylation. Also reported to stimulate glycogen synthesis and gene transcription and have protective effects on the heart and nerves. SB 431542, 98.0+ % (HPLC) 192-16541 5 mg 198-16543 25 mg for Cell Culture 331752-47-7 DMSO Keep at -20℃. IC50 of ALK = 7 nM <Protein kinase inhibitor> Selective inhibitor of activin receptor-like kinase (ALK) 4, 5 and 7 (the TGF-β type I receptor). Promotes proliferation, differentiation and sheet formation of endothelial cells of ES cell origin. Can be able to grow dramatically efficiency reprogramming to Human iPS Cells when used with Thiazovivin and PD0325901. It also promotes the speed. SP 600125, 98.0+ % (HPLC) 197-16591 5 mg 193-16593 25 mg for Cellbiology 129-56-6 Acetone, DMSO IC50 of JNK1: 40 nM; JNK2: 40 nM; JNK3: 90 nM Keep at -20℃. <MAP kinase inhibitor> MAPK inhibitor and potent ATP-competitive inhibitor of the c-Jun N-terminal kinase (JNK) subfamily. Its selectivity to JNK exceeds 20 times that of ERK and p38 MAPK. It inhibits c-Jun phosphorylation and the expression of inflammatory genes such as COX-2, LI-2, IFN-γ, and TNF-α. It is neuroprotective in vivo. D-erythro-Sphingosine, 99+% (TLC) 192-11161 25 mg for Biochemistry 123-78-4 MethanolIC50 of PKC: 1 - 3 μM chloroform mixture Keep at -20℃. <Protein kinase inhibitor / PTK inhibitor> Selective PKC inhibitot. It exhibit inhibitory action competitively to diacylglycerol, phorbol dibutyrate and Ca2+. It does not affect the activities of MLCK and PKA. It has also been reported to induce apoptosis in human myelocytic leukemia cells, HL-60. SR 3677 Hydrochloride, 98.0+ % (HPLC) 195-16151 2 mg for Cellbiology 1072959-67-1 Water, DMSO IC50 of ROCK-I: 56 nM, ROCK-II: 3 nM Keep at RT. 62996-74-1 DMSO IC50 of PKC: 2.7 nM; PKA: 8.2 nM; p60v-src tyrosine kinase: 6.4 nM Keep at -20℃. <Protein kinase inhibitor> Potent ROCK inhibitor Staurosporine, 95.0+ % (HPLC) 197-10251 100 μg 193-10253 500 μg for Biochemistry <PKC inhibitor / CDK inhibitor> A microbial alkaloid and extremely potent inhibitor of protein kinase Cs (PKCs). Also has comparable inhibitory actions on cAMP-dependent protein kinases (PKAs) and p60v-src tyrosine kinase, the product of an oncogene src. Stellettamide A Trifluoroacetate, 95.0+ % (HPLC) 193-11831 100 μg for Biochemistry 129744-24-7 Methanol - Keep at -20℃. <PKC inhibitor> Substance isolated and extracted from sponge (Stelletta sponge). It inhibits calmodulin. 9 1. Kinase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in for Cellbiology - Ethanol IC50 Storage Condition Summary SU 4312, 97.0+ % (HPLC) 190-15861 5 mg Ki: unactivated form: 0.04 μM; activated form: 4 μM Keep at -20℃. <Protein kinase inhibitor / Akt inhibitor> VEGFR2 tyrosine kinase inhibitor. Also Inhibits angiogenesis in tumors. SU 5402, 95.0+ % (HPLC) 193-16071 1 mg for Cellbiology 215543-92-3 DMSO - Keep at -20℃. <PTK inhibitor> Tyrosine kinase inhibitor in fibroblast growth factor receptor 1 (FGFR1). It also inhibits phosphorylation of ERK1 and ERK2 induced by aFGF. A recent study has demonstrated inhibition of differentiation at a high efficiency by incubating ES cells in a medium containing CHIR99021, SU5402 and PD184352. SU 5416, 97.0+ % (HPLC) 196-15841 5 mg for Cellbiology 204005-46-9 Ethanol IC50 of VEGFR2: 1.3 μM; FGFR1: 4.2 μM; PDGFRβ: 37.9 μM Keep at -20℃. <Protein kinase inhibitor / Akt inhibitor> VEGFR2 tyrosine kinase inhibitor. Also Inhibits angiogenesis in tumors. SU 6668, 98.0+ % (HPLC) 193-15851 5 mg for Cellbiology 252916-29-3 Ethanol IC50 of VEGFR2: 3.9 μM; FGFR1: 3.8 μM; PDGFRβ: 0.10 μM Keep at 2 - 10℃ 658084-23-2 - IC50 of c-MET tyrosine kinase: 10 nM; VEGFR1/2 tyrosine kinase: 0.8 mM; PDGFR: 19.4 mM Keep at -20℃. 54965-24-1 Ethanol IC50 of PKC: 2.7 nM; PKA: 8.2 nM; p60v-src tyrosine kinase: 6.4 nM Keep at 2-10℃. <Protein kinase inhibitor> VEGFR2 tyrosine kinase inhibitor SU 11274, 95.0+ % (HPLC) 198-17121 5 mg for Cellbiology 194-17123 25 mg <Protein kinase inhibitor> Selective inhibitor of c-MET tyrosine kinase. Tamoxifen Citrate, 98.0+ % (Ti) 209-14361 250 mg 205-14363 1g 203-14364 5g 207-14362 25 g for Biochemistry <PKC inhibitor> Estrogen analog, which is used as a drug used for prophylactic therapy of breast cancer, is known to selectively bind to estrogen receptors and is also called SERM (selective estrogen receptor modifier). It is considered to be deeply associated with diseases such as breast cancer and osteoporosis. Triciribine, 95.0+ % (HPLC) 206-19371 5 mg for Cellbiology 35943-35-2 - IC50 of AKT kinase: 150 nM Keep at -20℃. <Protein kinase inhibitor> Triciribine is inhibitor of AKT1/2/3 kinase and DNA synthesis inhibitor. TWS 119, 90.0+ % (HPLC) 206-17671 1 mg 202-17673 5 mg for Cellbiology 601514-19-6 Methanol - Keep at 2 - 10℃ <Protein kinase inhibitor> Acts as a potent and selective inhibitor of GSK-3β. Also reported to selectively induce neuronal differentiation in murine embryonic stem cells. Tyrphostin A25, 95.0+ % (HPLC) 204-19311 10 mg 200-19313 50 mg for Cellbiology 118409-58-8 - IC50: 3 μM Keep at -20℃. <Protein kinase inhibitor> EGFR tyrosine kinase inhibitor 10 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name CAS No. Soluble in IC50 Storage Condition 109511-58-2 Acetonitrile, ethanol - Keep at -20℃. Grade Summary U 0126 (mixture of isomers), 95.0+ % (HPLC) 211-01051 5 mg for Biochemistry <MAP kinase inhibitor> MAPK inhibitor used for signal transduction studies. 1. Kinase Inhibitors Wako Cat. No. Pkg. Size W-5 Hydrochloride 236-01721 5 mg 232-01723 25 mg for Biochemistry 61714-25-8 Methanol, water IC50 of PDE: 240 μM; MLCK: 230 μM Keep at -20℃. <PKC inhibitor / Calmodulin antagonist> A naphthalenesulfonate amide calmodulin antagonist to inhibit Ca2+/calmodulin-dependent phosphodiesterase (PDE) and myosin light chain kinase (MLCK). However, compared to W-7, its action as a calmodulin antagonist is low, and the product is mainly used as a negative control of W-7. W-7 Hydrochloride 233-01731 5 mg 239-01733 50 mg 237-01734 250 mg for Biochemistry 61714-27-0 Methanol, water IC50 of PDE: 28 μM; MLCK: 51 μM Keep at -20℃. <Protein kinase inhibitor / Calmodulin antagonist> A naphthalenesulfonate amide calmodulin antagonist to inhibit Ca2+/calmodulin-dependent phosphodiesterase and myosin light chain kinase. (+)-Wortmannin, 97.0+ % (HPLC) 230-02341 2 mg 236-02343 10 mg for Cellbiology 19545-26-7 Ethanol - Keep at -20℃. <Akt inhibitor> Has selective and irreversible inhibitory actions on myosin light chain kinases, a type of protein kinase that regulates smooth muscle contraction etc., and concentration-dependent and irreversible inhibitory actions on phosphatidylinositol 3-kinases, which are involved in phosphatidylinositol metabolism, one of the intracellular signal transduction mechanisms. Y-27632, 98.0+ % (HPLC) 257-00511 1 mg 253-00513 5 mg 251-00514 25 mg for Cellbiology 146986-50-7 Water p160ROCK (Ki = 140 nM) Keep at -20℃. <Protein kinase inhibitor> Selective and potent ROCK inhibitor. It inhibits contraction of the vascular smooth muscle, infiltration of cancer cells, and regulation of cell differentiation caused by a signal transduction system of ROCK. Enhances survival rate after cryopreservation and cloning efficiency of human ES and iPS cells. 5 mmol/L Y-27632 Solution 253-00591 300 μL for Cell Culture 331752-47-7 - - Keep at -20℃. <Protein kinase inhibitor> 5 mmol/L Y-27632 in aqueous soution. 11 2. Protein Phosphatase Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary 2. Protein Phosphatase Inhibitors Calyculin A, 95.0+ % (HPLC) 038-14453 10 μg 032-14451 100 μg for Biochemistry 101932-71-2 Methanol, ethanol, IC of PP2A: 3 nM; smooth muscle: 5 nM; DMSO smooth muscle endogenous: 1 nM Keep at -20℃. Contracts the smooth muscle regardless of the presence of external calcium, with its effects being approximately 100 times more potent than okadaic acid. A variety of actions have been confirmed, such as equally-potent inhibition of type 1 and 2A phosphatase activities and promotion of protein phosphorylation. Cantharidin 036-20461 25 mg 032-20463 100 mg 030-20464 500 mg for Cellbiology 56-25-7 Acetone IC50 of PP2A: 40 nM; PPA: 473 nM Keep at 2-10℃. Potent and selective protein phosphatase 2A inhibitor. Also inhibits protein phosphatase 1 at high concentrations. Cyclosporin A, 97.0+ % (HPLC) 031-18963 50 mg 035-18961 200 mg for Cellbiology 59865-13-3 Methanol, ethanol, acetone, ether, chloroform - Keep at 2-10℃. It is a representative immunosuppressant used for prevention of rejection reaction at the time of organ transplantation and it binds to the intracellular receptor in T lymphocytes inhibiting IL-2 and IFN-γ transcription (calcineurin inhibition). Consequently, it inhibits activation and proliferation of helper T cells contributing to immune reaction. Fostriecin Sodium Salt 065-05051 10 μg for Cellbiology 87860-39-7 Ethanol, water IC50 of PP1: 131 nM; PP2A: 3.2 nM Keep at -20℃. An antibiotic with anti-tumor activity isolated from Streptomyces pulveraceous (subspecies fostreus). Binds near the active center of the catalytic subunit of PP2A and inhibits substrate dephosphorylation. Does not affect PP2B enzyme activity but shows inhibitory action on PP1 as well at high concentrations. RK-682, 95.0+ % (HPLC) 185-01341 1 mg for Biochemistry - Ethanol, acetone IC50 of CD45: 54 μM; VHR: 2.0 μM Keep at RT. Specific tyrosine phosphatase inhibitor, which inhibits dephosphorylation of CD45 or VHR, protein-tyrosine phosphatase (PTPase), and regulates the cell cycle from G1 to S period. Tautomycin 209-12041 100 μg for Biochemistry 109946-35-2 Chloroform, ethanol, methanol IC50 of PP2A, PP1 (smooth muscle): 32 nM; PP1 (skeletal muscle): 22 nM; Smooth muscle endofenous: 6 nM Keep at -20℃. Protein phosphatase inhibitor and antifungal antibiotic produced from Streptomyces spiroverticillatus. Disodium β-Glycerophosphate Pentahydrate, 95.0+ % (Titration) 046-31251 50 g 042-31253 250 g for Cellbiology 13408-09-8 Water: 1 g/20 mL - Keep at 2-10℃. Has a structure of phosphorylated glycerol and in animal tissues is released into the blood with the breakdown of triglycerides in the liver. Also produced as a glycolytic intermediate. Levamisole Hydrochloride, 98.0+ % (Titration) 123-04641 10 g for Biochemistry 16595-80-5 Water: 210 g/L (20℃) - Keep at RT. Powder type of alkaline phosphatase inhibitor. It promotes the maturation of T lymphocytes and increases cellular immune responses. 12 for other products, please visit the Wako Online Catalog www.e-reagent.com 3. Inhibitor Cocktail Sets Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition - - Keep at 2-10℃. Summary Phosphatase Inhibitor Cocktail Solution I (×100) 167-24381 1 mL for Cellbiology - 5 phosphatase inhibitor mixture [Inhibition Target] serine/threonine phosphatases, tyrosine phosphatases, and dual-specificity phosphatases [Composition] sodium fluoride, sodium orthovanadate, sodium pyrophosphate, β-glycerophosphate, and sodium molybdate Phosphatase Inhibitor Cocktail Solution II (×100) 160-24371 1 mL for Cellbiology - - - Keep at 2-10℃. 5 phosphatase inhibitor mixture [Inhibition Target] acid phosphatases; alkaline phosphatases; tyrosine phosphatases [Composition] sodium fluoride, sodium tartrate, sodium orthovanadate, imidazole, and sodium molybdate Protease Inhibitor Cocktail Set I, Animal-derived-free (for general use) (x 100), Lyophilized for 1 mL 161-26023 for 1 mL x 5 for Cellbiology - - - Keep at -20℃. 5 inhibitor mixture solution. It replaces aprotinin from bovine lung with recombinant aprotinin produced with no animal by-products. [Inhibition Target] a wide variety of proteases and esterases. Protease Inhibitor Cocktail Set III, DMSO Solution (EDTA free) (x 100) 163-26061 1 mL 169-26063 1 mL x 5 for Cellbiology - - - Keep at -20℃. 3. Inhibitor Cocktail Sets 165-26021 6 inhibitor mixture solution being suitable for experiments targeted on metal-binding proteins in mammalian cells, tissue extracts, and bacterial extracts. It does not contain EDTA or other metalloproteinase inhibitors. [Inhibition Target] a wide range of proteases including aminopeptidases. Protease Inhibitor Cocktail Set III, DMSO Solution, Animal-derived-free (EDTA free) (×100) 160-26071 1 mL 166-26073 1 mL x 5 for Cellbiology - - - Keep at -20℃. 6 inhibitor mixture solution being suitable for experiments targeted on metal-binding proteins in mammalian cells, tissue extracts, and bacterial extracts. It inhibits a wide range of proteases including aminopeptidases. It does not contain EDTA or other metalloproteinase inhibitors. It replaces aprotinin from bovine lung with recombinant aprotinin produced with no animal by-products. Protease Inhibitor Cocktail Set IV, DMSO Solution (for Fungal and Yeast) (×100) 167-26081 1 mL 163-26083 1 mL x 5 for Cellbiology - - - Keep at -20℃. - Keep at -20℃. 4 inhibitor mixture DMSO solution, being suitable for use in mold and yeast extracts. [Inhibition Target] serin proteases, cystein proteases, metalloproteases, asparatic proteases. Protease Inhibitor Cocktail Set V (EDTA free) (×100), Lyophilized 162-26031 for 1 mL 168-26033 for 1 mL x 5 for Cellbiology - - 4 inhibitor mixture solution, being suitable for experiments targeted on metal-binding proteins and recombinant proteins. In addition, also useful for metal-affinity column chromatography. [Inhibition Target] serin proteases, cystein proteases, metalloproteases, asparatic proteases. Protease Inhibitor Cocktail Set VI, DMSO Solution (for Plant) (×100) 164-26091 1 mL 160-26093 1 mL x 5 for Cellbiology - - - Keep at -20℃. 6 inhibitor mixture solution, being suitable for plant extracts. [Inhibition Target] serin proteases, cystein proteases, trypsin-like proteases, aminopeptidase B, leucine aminopeptidase, asparatic proteases, metalloproteases. Protease Inhibitor Cocktail Set VII, DMSO Solution (for Histidine-tagged Protein) (× 100) 167-26101 1 mL 163-26103 1 mL x 5 for Cellbiology - - - Keep at -20℃. EDTA-free 5 inhibitor mixture solution, being suitable for purification of histidine-tagged proteins. [Inhibition Target] serin proteases, cystein proteases, aminopeptidase B, leucine aminopeptidase, asparatic proteases, metalloproteases. 13 4. Calcium Signaling related Inhibitors Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary Alendronate Sodium Salt Trihydrate, 97.0+ % (HPLC) 012-22661 100 mg 018-22663 500 mg for Pharmacology Research 121268-17-5 Water IC50 = 10 μM Keep at -20℃. <Calcium metabolism regulator> This product is a bisphosphonate compound that is selectively distributed in the calcified bone surface to which the osteoclasts are attached. It is released under an acid environment created by the osteoclasts, taken in the cells, and inhibits the bone resorption activity. The inhibition of the bone resorption is considered to be caused by apoptosis induction effect of the osteoclasts and direct suppression of bone resorption of the osteoclasts. (-)-Blebbistatin, 98.0+ % (HPLC) 021-17041 1 mg 027-17043 5 mg for Cellbiology 856925-71-8 DMSO (5 mg/mL) - Keep at -20℃. <Calcium ATPase Inhibitors> Specific inhibitor of myosin II. It inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly in the vertebrate cell divisions. It has been reported to block blebbing and apoptosis and increases the colony forming rate when human ES cells are dispersed to single cells from a colony. Calpain Inhibitor 2, 95.0+ % (HPLC) 038-19811 10 mg for Cellbiology 110115-07-6 Ethanol, methanol - Keep at -20℃. 4. Calcium Signaling related Inhibitors <Calpain inhibitors> This product inhibits neutral cysteine proteinases such as calpain 1, calpain 2, cathepsin B and cathepsin L. It is also a weak inhibitor of proteasomes. Chlorpromazine Hydrochloride, 99.0+ % (Titration) 033-10581 10 g for Biochemistry 69-09-0 Water, ethanol IC50 = 25 μM Keep below 25℃. <Calmodulin antagonists> Chlorpromazine Hydrochloride is a phenothiazine neuroleptic which induces tranquilization, analgesia, lowering of body temperature by inhibiting the hypothalamic thermoregulatory mechanism, antiemesis by inhibiting CTZ of the medulla oblongata, inhibition of conditioned avoidance response, and hypnosis, as well as an antidopaminergic. This reagent potently blocks α-adrenergic receptors. Its mode of action in the biogenic system is inhibition of calmodulin, similar to trifluoperazine. Cyclopiazonic Acid, 98.0+ % (HPLC) 030-17171 5 mg for Biochemistry 18172-33-3 Methanol IC50 of Ca2+: 0.2 μM; ATPase: 0.35 μM Keep at -20℃. <Calcium ATPase Inhibitors> Mycotoxin (fungal toxin). It is a specific inhibitor of Ca2+-ATPase. 2,5-Di-t-butylhydroquinone, 99.0+ % (Capillary GC) 040-24681 100 mg for Biochemistry 046-24683 88-58-4 1g Benzene,ethanol, acetone, IC50 = 66.7 ± 2.1 μM carbon bisulfide Keep at RT. <Calcium ATPase Inhibitors> This product inhibits the Ca2+ ATPase of the sarcoplasmic reticulum and does not act on the plasma membrane Ca2+ pump. E-64d, 97.0+ % (HPLC) 054-08021 1 mg 050-08023 5 mg for Cellbiology 88321-09-9 Methanol IC50 = 0.5 μM Keep at -20℃. <Calpain inhibitors> Membrane-permeable cysteine protease inhibitor which is an analog of E-64, a cysteine protease inhibitor isolated from Aspergillus japonicas. Esters are hydrolyzed when permeated through the membrane and E-64d is considered to change to an activated form, E-64c. This reagent inhibits calpain and cathepsin. It is used in combination with pepstatin A in order to prevent degradation of LC3-II in the autophagosome inner membrane during autophagy. Fluphenazine Dimaleate, 98.0+ % (Titration) 061-01751 1g for Biochemistry 3093-66-1 Dilute hydrochloric acid - Keep at 2-10℃. <Calmodulin antagonists> Phenothiazine neuroleptic. It is a calmodulin inhibitor, similar to chlorpromazine. 14 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in for Cellbiology 72093-21-1 Water IC50 Storage Condition Summary Mastoparan 139-16511 1 mg IC50 = 15 μM Keep at -20℃. <Calmodulin antagonists> Amphiphilic peptide isolated as an ingredient of hornet poison. It activated directly pertussis toxin-sensitive G protein (Gi, G0) by a mechanism resembling G protein-conjugate type receptors. It also acts as a calmodulin antagonist. MG-132, 80.0+ % (HPLC) 139-16251 1 mg 135-16253 5 mg for Cellbiology 133407-82-6 Methanol IC50 = 1.25 μM Keep at -20℃. <Calpain inhibitors> Membrane-permeable peptide aldehyde protease inhibitor which reversibly inhibits the chymotrypsin-like activity of 26S proteasome. Quinacrine Dihydrochloride Dihydrate, 95.0+ % (HPLC) 171-00502 25 g for Biochemistry 69-05-6 Water, ethanol IC50 = 4.4 μM Keep below 25℃. <Calmodulin antagonists> Antimalarial; calmodulin inhibitor; phospholipase inhibitor Suramin Sodium, 98.0+ % (HPLC) 199-10613 100 mg 193-10611 200 mg for Biochemistry 129-46-4 Water IC50 = 4.9 ± 1.2 μM Keep at RT. <Calcium ATPase Inhibitors> This product inhibits Ca2+ ATPase of the sarcoplasmic reticulum. It also blocks growth factors, including EGF from binding to the cell envelope. 209-17281 1 mg 205-17283 5 mg for Cellbiology 67526-95-8 Acetonitrile IC50 = 0.13 ± 0.02 μM Keep at -20℃. <Calcium ATPase Inhibitors> Thapsigargin is an endoplasmic reticulum Ca2+-ATPase(SERCA) inhibitor which inhibits all SERCA isoforms. The endoplasmic reticulum uptake of calcium ion is blocked causing releasing of calcium ions from the endoplasmic reticulum to the cytoplasm, by irreversible inhibition of SERCA activity. 4. Calcium Signaling related Inhibitors Thapsigargin 5. Ion Channel-related Blockers 5. Ion Channel-related Blockers (1) Calcium Channel Blockers Product Name Wako Cat. No. Pkg. Size Manufacturer CAS No. Soluble in IC50 Storage Condition - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. Summary ω-Agatoxin IVA (P-type Blocker), from Funnel Web Spider, Agelenopsis aperta 339-42561 0.1 mg Peptide Institute, Inc. (4256-s) 145017-83-0 - Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers. ω-Agatoxin TK (P-type Blocker) 339-42941 0.1 mg Peptide Institute, Inc. (4294-s) 145017-83-0 - Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers. Agelenin, from Spider, Agelena opulenta 330-42471 0.1 mg Peptide Institute, Inc. (4247-s) - - Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers. 15 Product Name Wako Cat. No. Pkg. Size Grade/Manufacturer CAS No. Soluble in IC50 Storage Condition 88150-42-9 - - Keep at RT. Summary Amlodipine, 98.0+ % (HPLC) 011-24951 100 mg 017-24953 1g for Cellbiology L-type calcium channel blocker with a hypotensive action. It acts on cardiovascular system, including facilitation of NO production, inhibition of oxidative stress, and inhibition of adhesion of monocytes to the endothelium. In addition, it acts for a prolonged period compared to other similar calcium channel blockers. 2,3-Butanedione Oxime 045-00652 25 g 047-00651 100 g Wako Special Grade 57-71-6 Water, ethanol IC50 = 15.3 mM Keep at RT. 2,3-Butanedione Oxime has phosphatase activity and inhibits contraction of skeletal muscles and cardiac muscles. Calcicludine (L-type Blocker), 99.0+ % (HPLC), from Green Mamba, Dendroaspis angusticeps 337-43101 0.1 mg Peptide Institute, Inc. (4310-s) 178037-96-2 - - Keep at -20℃. - Keep at -20℃. Neuronal L-type Ca2+ Channel Blocker. Peptidic ion channel blockers. Calciseptine (L-type Blocker), from Black mamba, Dendroaspis polylepis polylepis 332-42551 0.1 mg Peptide Institute, Inc. (4255-s) - - L-type Ca2+ Channel Blocker. Peptidic ion channel blockers. Cinnarizine, 98.0+ % (Titration) 030-13592 25 g for Biochemistry Acetone, ether, chloroform, benzene 298-57-7 IC50 = 0.75 μM Keep at RT. Cinnarizine has antihistaminic and vasodilatory activities, improves cerebral blood flow impairment, and exerts Ca2+ channel inhibitory activity. ω-Conotoxin GVIA (N-type Blocker), from Marine Snail, Conus geographus 5. Ion Channel-related Blockers 336-41611 0.5 mg Peptide Institute, Inc. (4161-v) 106375-28-4 - - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. N-type Ca2+ Channel Blocker. Peptidic ion channel blockers. ω-Conotoxin MVIIA (N-type Blocker), 99.0+ % (HPLC) from Marine snail, Conus magus 338-42891 0.5 mg Peptide Institute, Inc. (4289-v) 107452-89-1 - Reversible N-type Ca2+ Channel Blocker. Peptidic ion channel blockers. ω-Conotoxin MVIIC (P/Q-type Blocker), 99.0+ % (HPLC), from Marine Snail, Conus magus 332-42833 336-42831 0.5 mg Peptide Institute, Inc. (4283-v) 0.1 mg Peptide Institute, Inc. (4283-s) 147794-23-8 - P/Q-type Ca2+ Channel Blocker. Peptidic ion channel blockers. ω-Conotoxin SVIB (N-type Blocker), 99.0+ % (HPLC), from Marine Snail, Conus striatus 333-42841 0.5 mg Peptide Institute, Inc. (4284-v) 150433-82-2 - N-type Ca2+ Channel Blocker. Peptidic ion channel blockers. Diltiazem Hydrochloride, 98.0+ % (Titration) 047-20311 1g 043-20313 5g for Biochemistry 33286-22-5 Formic acid, water, ethanol, chloroform IC50 = 4.5 μM Keep at 2-10℃. Therapeutic substance for circulatory diseases such as hypertension, angina and arrhythmia. It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts. Specific calcium antagonists include nifedipine, verapamil and diltiazem. 16 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size Grade/Manufacturer CAS No. Soluble in IC50 Storage Condition - Keep at -20℃. Summary Kurtoxin, 98.0+ % (HPLC), from Scorpion, Parabuthus transvaalicus 338-43751 0.1 mg Peptide Institute, Inc. (4375-s) - - T-type Ca2+ channel blocker. Peptidic ion channel blockers. Nicardipine Hydrochloride, 99.0+ % (HPLC) 145-06381 1g 141-06383 5g for Biochemistry 54527-84-3 Methanol, chloroform IC50 = 2.56 μM Keep at RT. It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts. Nitrendipine, 98.0+ % (HPLC) 142-06411 200 mg for Biochemistry 39562-70-4 Chloroform, acetonitrile IC50 = 23 μM Keep at RT. It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts. It dilates peripheral vessels and coronary arteries and has hypotensive and anti-angina actions. Its hypotensive action is comparable to nifedipine, and the action lasts longer than nifedipine. PLTX-II, 99.0+ % (HPLC), from Spide, Plectreurys tristes 331-43001 0.1 mg Peptide Institute, Inc. (4300-s) - - - Keep at -20℃. - - Keep at -20℃. - Keep at -20℃. Presynaptic Ca2+ Channel Blocker ProTx-1, 97.0+ % (HPLC), from Tarantula, Thrixopelma pruriens 338-44091 0.1 mg Peptide Institute, Inc. (4409-s) - T-Type Ca2+ Channel / Na+ Channel / K+ Channel Blocker (Gating Modifier) Ryanodine 185-02821 1 mg for Cellbiology 15662-33-6 Methanol Signal transduction Ca channel Inhibitor Ryanodine is an alkaloid isolated from Ryania speciosa Vahl. It acts to increase calcium permeability by binding to the arcoplasmic reticulum calcium channel. 2+ 338-43631 0.1 mg Peptide Institute, Inc. (4363-s) 203460-30-4 - - Keep at -20℃. Class E (R-type) Ca2+ Channel Blocker Verapamil Hydrochloride, 98.0+ % (Titration) 222-00781 1g 228-00783 10 g for Biochemistry 152-11-4 Ethanol IC50 = 0.3 μM Keep at RT. 5. Ion Channel-related Blockers SNX-482, 99.0+ % (HPLC), from Tarantula, Hysterocrates gigas Verapamil HCl directly affects the smooth muscle of blood vessels and the heart and is a Ca2+ antagonist. It also promotes effects of tumoricidal drugs and is used in research concerning the mechanism of calcium antagonists. (2) Potassium Channel Blockers Product Name Wako Cat. No. Pkg. Size Manufacturer CAS No. Soluble in IC50 Storage Condition - - Keep at -20℃. - Keep at -20℃. Summary Apamin, 99.0+ % (HPLC), from Honeybee, Apis mellifera 336-42571 0.5 mg Peptide Institute, Inc. (4257-v) 24345-16-2 Small conductance Ca2+-activated K+ channel blocker Charybdotoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus var. hebraeus 338-42271 0.1 mg Peptide Institute, Inc. (4227-s) 95751-30-7 - Ca2+-activated K+ channel blocker 17 Product Name Wako Cat. No. Pkg. Size Grade/Manufacturer CAS No. Soluble in IC50 Storage Condition - Keep at -20℃. Summary Dendrotoxin 1, 99.0+ % (HPLC), from black mamba, Dednroaspis polylepis polylepis 339-43301 0.1 mg Peptide Institute, Inc. (4330-s) 107950-33-4 - - Water Voltage-dependent K+ channel blocker E-4031 n-Hydrate, 98.0+ % (HPLC) 059-08451 10 mg 055-08453 50 mg for Cellbiology Native guinea pig HERG channel: IC50 = 397 nM Keep at -20℃. E-4031 is a HERG potassium channel blocker with antiarrhythmic action (class III ). It selectively inhibits Ikr, a rapid component of the delayed rectifier K current, during repolarization after muscle cells are depolarized. Glibenclamide, 98.0+ % (Titration) 078-03881 5g 076-03882 25 g for Biochemistry 10238-21-8 DMF IC50 = 0.1 μM Keep at RT. <Potassium Channel Blockers> Sulfonylurea hypoglycemic substance. It blocks ATP-dependent K+ channel of the pancreas to increase intracellular Ca2+, thus increasing insulin secretion. It pharmacologically antagonizes the action of K+ channel-opening agents in the heart and blood vessels. Guangxitoxin-1E, 97.0+ % (HPLC), from Tarantula, Plesiophrictus guangxiensis sp. nov. 334-44331 0.1 mg Peptide Institute, Inc. (4433-s) - - Keep at -20℃. - Keep at -20℃. - - Keep at -20℃. - - Keep at -20℃. - - Keep at -20℃. - Keep at -20℃. - Kv2.1/Kv2.2 channel blocker / Enhancer of glucose-dependent insulin secretion Iberiotoxin, 99.0+ % (HPLC), from Scorpion, Buthus tamulus 330-42351 0.1 mg Peptide Institute, Inc. (4235-s) 129203-60-7 - Highly selective and potent high conductance Ca2+-activated K+ channel blocker Kaliotoxin (1-37), 99.0+ % (HPLC), from Scorpion, Androctonus mauretanicus mauretanicus 5. Ion Channel-related Blockers 330-42591 0.1 mg Peptide Institute, Inc. (4259-s) 145199-73-1 High conductance Ca2+-activated K+ channel blocker Margatoxin【MgTX】, 99.0+ % (HPLC) 331-42901 0.1 mg Peptide Institute, Inc. (4290-s) 145808-47-5 Voltage-dependent K+ channel blocker (specific for Kv1.3 channel ) MCD-Peptide, 99.0+ % (HPLC), from Honeybee, Apis mellifera 333-42581 0.5 mg Peptide Institute, Inc. (4258-v) 32908-73-9 Voltage-dependent K+ channel blocker Scyllatoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus hebraeus 333-42601 0.1 mg Peptide Institute, Inc. (4260-s) 116235-63-3 - Small conductance Ca2+-activated K+ channel blocker Stichodactyla Toxin, 99.0+ % (HPLC), from Sea Anemone, Stichodactyla helianthus 334-42871 0.1 mg Peptide Institute, Inc. (4287-s) - - - Keep at -20℃. 58694-52-3 - - Keep at -20℃. Voltage-dependent K+ channel (A channel) blocker Tertiapin, 99.0+ % (HPLC), from Apis mellifera 335-43641 0.1 mg Peptide Institute, Inc. (4364-s) Potent blocker of inward-rectifier K+ channels such as ROMK1 and GIRK1/4 at 2.5-10 nM. 18 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size CAS No. Manufacturer Soluble in IC50 Storage Condition - - Keep at -20℃. Soluble in IC50 Storage Condition Summary Tityustoxin Kα, 99.0+ % (HPLC), from Scorpion, Tityus serrulatus 338-43131 0.1 mg Peptide Institute, Inc. (4313-s) 39465-37-7 Voltage-dependent K+ channel (A channel) blocker (3) Sodium Channel Blockers Product Name Wako Cat. No. Pkg. Size CAS No. Grade/Manufacturer Summary Clotrimazole, 98.0+ % (HPLC) 035-16021 5g 033-16022 25 g for Biochemistry 23593-75-1 Ethanol, chloroform, IC50 = 1.8 μM carbon tetrachloride Keep at RT. It exhibits bactericidal action by destroying cytoplasmic membranes of fungi. μ-Conotoxin G3B, 99.0+ % (HPLC), from Marine Snail, Conus geographus 332-42171 0.5 mg Peptide Institute, Inc. (4217-v) 140678-12-2 - - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. Na+ channel blocker: Specific for skeletal muscle μ-Conotoxin GS, 95.0+ % (HPLC), from Marine Snail, Conus geographus 334-42631 0.5 mg Peptide Institute, Inc. (4263-v) 171358-00-2 - Selective blocker of Na+ channels of skeletal muscles. μ-Conotoxin SIIIA, 99.0+ % (HPLC), from Marine Snail, Conus striatus 339-44401 0.5 mg Peptide Institute, Inc. (4440-v) 877860-32-7 - Tetrodotoxin-resistant Na+ channel blocker with analgesic activity Huwentoxin-IV, 97.0+ % (HPLC), from Chinese Bird Spider, Ornithoctonus huwena 0.1 mg Peptide Institute, Inc. (4455-s) - - 73590-58-6 Dichloromethane, methanol Neuronal tetrodotoxin-sensitive Na+-channel blocker Omeprazole, 98.0+ % (HPLC) 150-02091 10 g 158-02092 25 g for Biochemistry IC50 = 4.2 μM Keep at -20℃. 5. Ion Channel-related Blockers 330-44551 Eradicating agent for Helicobacter pylori (HP). Selective inhibitor of gastric H+, K+ ATPase (proton pump), and used as a marker to test the susceptibility of HP to this product in vitro. ProTx-II, 99.0+ % (HPLC) 335-44501 0.1 mg Peptide Institute, Inc. 4450-s - - Keep at -20℃. CAS No. Soluble in IC50 Storage Condition 545395-94-6 Ethanol - Keep at 2-10℃. - Na+ channel (especially Nav1.7) / Ca2+ channel blocker (gating modifier) (4) Transient Receptor Potential (TRP) Channel Blockers Product Name Wako Cat. No. Pkg. Size Grade Summary AMG 9810, 98.0+ % (HPLC) 015-25071 10 mg 011-25073 50 mg for Cellbiology Antagonist of transient receptor potential vanilloid 1 (TRPV1). TRPV1 is one of the TRP channels cloned as a capsaicin receptor, functions as a pain receptor, and is activated by capsaicin, heat, and protons. It also inhibits the activation of TRPV1 by heat and protons, besides capsaicin. 19 Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition for Cellbiology 55224-94-7 Ethanol (10 mg/2 mL) - Keep at -20℃. Summary AP 18, 98.0+ % (HPLC) 014-25161 10 mg 010-25163 50 mg Selective TRPA1 (transient receptor potential ankyrin 1) inhibitor. TRPA1 is involved in pain transmission, and its involvement in respiratory depression has also been reported. 2-APB, 98.0+ % (HPLC) 013-24911 100 mg 019-24913 500 mg for Cellbiology 524-95-8 Ethanol - Keep at -20℃. Inhibitor of inositol triphosphate (IP3) receptors. It can also block TRP channels TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2. At high concentrations, it can activate TRPV1, TRPV2 and TRPV3. BCTC, 98.0+ % (HPLC) 027-18241 10 mg 023-18243 50 mg for Cellbiology 393514-24-4 Ethanol - Keep at -20℃. TRPV1 antagonist. It inhibits the activation of TRPV1 by capsaicin and acids. Capsazepine, 98.0+ % (HPLC) 037-23171 10 mg 033-23173 50 mg for Cellbiology 138977-28-3 Ethanol - Keep at 2-10℃. 349085-38-7 DMSO - Keep at RT. Ethanol - Keep at -20℃. TRPV1 antagonist. Capsaicin analog. HC-030031, 98.0+ % (HPLC) 086-09961 10 mg 082-09963 50 mg for Cellbiology Selective TRPA1 (transient receptor potential ankyrin 1) inhibitor. 5. Ion Channel-related Blockers Olvanil, 98.0+ % (HPLC) 154-03231 10 mg 150-03233 50 mg for Cellbiology 58493-49-5 It demonstrated to block intracellular accumulation of Anandamide through interaction with the anandamide transporter at concentrations similar to those needed for TRPV1 activation. Also inhibits FAAH (fatty acid amide hydrolase). It also acts as a potent TRPV1 angonist and a CB1 agonist. RN-1747, 98.0+ % (HPLC) 183-02981 10 mg 189-02983 50 mg for Cellbiology 1024448-59-6 DMSO - Keep at 2-10℃. TRPM8 antagonist. It also acts as a TRPV4 (transient receptor potential vanilloid 4)-selective agonist. Ruthenium Red 184-00331 100 mg 180-00333 1g Wako Special Grade 11103-72-3 Water - Keep at RT. 472981-92-3 Ethanol - Keep at -20℃. TRPA1 antagonist. SB-366791, 98.0+ % (HPLC) 193-17431 10 mg 199-17433 50 mg for Cellbiology TRPV1 antagonist, which inhibits the activation of TRPV1 by capsaicin and heat. It has been reported that it does not inhibit activation by protons. 20 for other products, please visit the Wako Online Catalog www.e-reagent.com (5) Acid-Sensing Ion Channel Blockers Product Name Wako Cat. No. Pkg. Size Manufacturer CAS No. Soluble in IC50 Storage Condition 713544-47-9 - - Keep at -20℃. Summary APETx2, 99.0+ % (HPLC) 331-44721 0.1 mg Peptide Institute, Inc. (4472-s) Selective blocker of acid-sensing ion channel blocker, ASIC3 Psalmotoxin 1, 97.0+ % (HPLC), from South American Tarantula, Psalmopoeus cambridgei (Trifluoroacetate Form) 338-44351 0.1 mg Peptide Institute, Inc. (4435-s) - - - Keep at -20℃. Soluble in IC50 Storage Condition Selective blocker of ASIC1a (6) Nicotinic Acetylcholine Receptor Blockers Product Name Wako Cat. No. Pkg. Size Manufacturer CAS No. Summary α-Conotoxin G1, 97.0+ % (HPLC), from Marine Snail, Conus geographus (Hydrochloride Form) 337-41261 0.5 mg Peptide Institute, Inc. (4126-v) 76862-65-2 - - Keep at -20℃. - Keep at -20℃. - Keep at -20℃. Nicotinic acetylcholine receptor blocker α-Conotoxin ImI, 99.0+ % (HPLC), from Marine Snail, Conus imperialis 334-43111 0.5 mg Peptide Institute, Inc. (4311-v) 156467-85-5 - Nicotinic acetylcholine receptor blocker in central nervous system α-Conotoxin M1, 99.0+ % (HPLC), from Marine Snail, Conus magus 337-41401 0.5 mg Peptide Institute, Inc. (4140-v) 88217-10-1 - Nicotinic acetylcholine receptor blocker 335-42281 0.5 mg Peptide Institute, Inc. (4228-v) 133605-58-0 - - Keep at -20℃. CAS No. Soluble in IC50 Storage Condition Nicotinic acetylcholine receptor blocker (7) Other Blockers Product Name Wako Cat. No. Pkg. Size Manufacturer 5. Ion Channel-related Blockers α-Conotoxin SI, 99.0+ % (HPLC), from Marine Snail, Conus striatus Summary Chlorotoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus 339-42821 0.5 mg Peptide Institute, Inc. (4282-v) 163515-35-3 - - Keep at -20℃. - - - Keep at -20℃. - Keep at -20℃. Small-conductance Cl- channel blocker GsMTx-4, 99.0+ % (HPLC) 336-43931 0.1 mg Peptide Institute, Inc. (4393-s) Inhibitor for cation-selective stretch-activated channels / Atrial fibrillation inhibiting peptide Purotoxin-1, 99.0+ % (HPLC) 334-44571 0.1 mg Peptide Institute, Inc. (4457-s) - - P2X3 purinoreceptor inhibitor 21 6.G-protein Signaling and Second Messenger-related Inhibitors Product Name Wako Cat. No. Pkg. Size CAS No. Grade/Manufacturer Soluble in IC50 Storage Condition Summary Andrographolide, 98.0+ % (HPLC) 014-15271 500 mg for Biochemistry 5508-58-7 Methanol, acetone IC50 = 5.6 ± 0.7 μM Keep at 2-10℃. <Guanylate Cyclase Inhibitors> It is reported to suppress the decrease of glutathion and to counteract toxic liver damage caused by substances such as carbontetrachloride and t-butylhydroperoxide. BAY 11-7085, 98+ % (NMR) 020-14331 10 mg 026-14333 25 mg for Biochemistry 196309-76-9 Ethanol, acetone IC50 = 10 μM Keep at -20℃. <NFκB Inhibitors> Inhibitor of cytokine-induced IκBα phosphorylation and decreases expression of NFκB and adhesion molecule. It also exhibits strong antiinflammatory activity. 8-(4-Chlorophenylthio)adenosine 3',5'-(Cyclic)monophosphate Sodium Salt, 98.0+ % (HPLC) 039-18121 10 mg 035-18123 100 mg for Biochemistry 93882-12-3 Water IC50 of PKA: 900 nM; PKG: 25 μM Keep at -20℃. <Adenylate Cyclase Inhibitors> Cell permeable cAMP analog, used as an activator of cAMP-dependent protein kinase (PKA) and cGMP-dependent protein kinase (PKG). Curcumin 038-04921 1g 036-04922 25 g Wako Special Grade IC50 of 5-Lipoxygenase: 5 - 10 μM, COX ≦ 100 μM 458-37-7 Ethanol, acetic acid 477-57-6 - - Keep at 2-10℃. Ethanol, acetone IC50 of soluble Guanylate cyclase in human platelets: 2 μM; leukotriene synthesis in guinea pig lung and rat celiac cells: 1.8 μM Keep at -20℃. Keep at RT. <Guanylate Cyclase Inhibitors> Inhibitor of 5-lipoxygenase and cyclooxygenase. Isotetrandrine 306-01771 25 mg Kaken Shoyaku Co., Ltd. <G-protein Signaling Inhibitor> A biscoclaurine alkaloid inhibitor of G protein activation of PLA2 LY-83583, 94+ % (TLC) 128-04691 5 mg for Biochemistry 91300-60-6 <Guanylate Cyclase Inhibitors> It decreases the concentration of cellular cGMP through the inhibition of guanylate cyclase. NS2028, 98.0+ % (HPLC) 6. G-protein Signaling and Second Messenger-related Inhibitors 149-06921 5 mg for Biochemistry 204326-43-2 Water, ethanol - Keep at -20℃. <Guanylate Cyclase Inhibitors> Selective inhibitor of soluble guanylate cyclase (sGC) that is sensitive to NO. It does not inhibit sGC activity enhanced by YC-1 or CO. 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one【ODQ】, 97.0+ % (HPLC) 153-01981 10 mg 159-01983 25 mg for Biochemistry 41443-28-1 Ethanol, acetone - Keep at 2-10℃. <Guanylate Cyclase Inhibitors> It inhibits the guanylate cyclase activity of NO produced by NOS rather than NO synthase (NOS), and controls the increase in cGMP. Pentoxifylline, 98.0+ % (Titration) 160-18761 10 g for Biochemistry 6493-05-6 Methanol, ethanol, TNFα: IC50 = 100 μM acetone, water Keep at RT. <Guanylate Cyclase Inhibitors> TNF-α synthesis inhibior and phosphodiesterase inhibitor 22 for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in for Biochemistry 61413-54-5 Ethanol IC50 Storage Condition Summary Rolipram, 98+ % (TLC) 180-01411 10 mg IC50 = 20 μM Keep at 2-10℃. <NFκB Inhibitors> This cAMP diphosphodiesterase inhibitor selectively inhibits phosphodiesterase IV, a type of isozyme. Improvement of arthritis (in rats with collagen II induced arthritis) has been reported. 7.Neurotransmitter Inhibitors (1) Glutamate Receptor Antagonists Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Hydrochloric acid, water - Keep at 2-10℃. Summary DL-2-Amino-4-phosphonobutyric Acid, 98.0+ % (HPLC) 013-22071 100 mg for Cellbiology 6323-99-5 NMDA-type glutamate receptor antagonists. L-2-Amino-4-phosphonobutyric Acid, 98.0+ % (HPLC) 016-22083 10 mg for Cellbiology 23052-81-5 Water EC50 = 16.0 μM Keep at 2-10℃. Selective agonist for group III metabotropic glutamate receptors ( mgluR4, mgluR6). D(-)-2-Amino-5-phosphonovaleric Acid 【D-AP5】 015-18481 10 mg for Biochemistry 79055-68-8 Hydrochloric acid IC50 = 3.7 ± 0.32 μM Keep at RT. A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors. DL-2-Amino-5-phosphonovaleric Acid 【DL-AP5】 018-18471 10 mg for Biochemistry 76326-31-3 Water IC50 = 90 μM Keep at RT. A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors. (R)-CPP 031-22091 1 mg 037-22093 5 mg for Cellbiology 126453-07-4 Water (10 mg/mL) - Keep at RT. Highly potent glutaminergic NMDA receptor antagonist. It exhibits a higher activity than racemic CPP. It is selective to NR2A in NMDA receptor. Dextromethorphan Hydrobromide Monohydrate, 98.0+ % (Titration) 041-21551 5g 049-21552 25 g for Biochemistry Methanol, acetic acid, ethanol - Keep below 25℃. 364-98-7 DMSO - Keep at RT. 85797-13-3 NaOH soln. IC50 = 11.1 ± 2.1 μM Keep at RT. NMDA receptor antagonist. Diazoxide, 99.0+ % (HPLC) 047-23133 250 mg 041-23131 1g for Biochemistry Desensitization blocker of AMPA receptor. DL-AP7, 98.0+ % (1H- NMR) 041-31941 5 mg for Cellbiology DNQX, 95+ % (TLC) 044-26301 50 mg for Biochemistry AMPA/Kainate receptor antagonist 2379-57-9 Methanol - Keep at -20℃. 7. Neurotransmitter Inhibitors A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors. 6. G-protein Signaling and Second Messenger-related Inhibitors 6700-34-1 23 Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in Practical Grade 314-13-6 Water 25451-15-4 DMSO, ethanol IC50 Storage Condition Summary Evans Blue 056-04061 5g 054-04062 25 g IC50 = 87 nM Keep at RT. AMPA/Kainate receptor antagonist. Felbamate, 98.0+ % (HPLC) 060-05861 10 mg 066-05863 50 mg for Cellbiology IC50 = 0.78 ± 0.07 mM Keep at -20℃. Allosteric antagonist of NR2B subunit of glutaminergic NMDA receptor and exhibits strong anticonvulsant action. It also has a property as a γ-aminobutyric acid (GABA) receptor agonist. Joro Spider Toxin JSTX-3, 98.0+ % (HPLC) 104-00051 0.1 mg for Biochemistry 112163-33-4 Water IC50 = 1.7 μM Keep at 2-10℃. Toxin isolated from Joro Spider poison gland, paralyzes the movement of arthropods (insects, crustaceans, etc.). It irreversibly blocks excitatory transmissions of neurons and muscles by glutamate released from the synaptic terminal of motor neurons. It acts selectively on quisqualate glutamate receptor. Loperamide Hydrochloride 129-05721 5g 127-05722 25 g for Pharmacology Research 34552-83-5 Methanol, ethanol IC50 = 0.9 ± 0.2 μM Keep at RT. NMDA receptor antagonist. It reduces Ca2+ flow. Loperamide Hydrochloride is a NMDA receptor antagonist that reduces the flow of Ca2+. It is an antidiarrheal agent that inhibits both peristaltic movement of the intestinal tract and secretion, and enhances absorption, via opioid receptor in the intestinal tract. (+)-MCPG, 99.0+ % (HPLC) 135-16111 2 mg 131-16113 10 mg for Cellbiology 150145-89-4 0.1M NaOH IC50 = 272 μM Keep at 2-10℃. Competitive antagonist for group 1 (mGluR1, mGluR5) and group 2 (mGluR2, mGluR3) metabotropic glutamate receptors. It is an active enantiomer of (±)-MCPG. Memantine Hydrochloride 132-16981 25 mg 138-16983 100 mg for Cellbiology 41100-52-1 Water IC50 = 1.2 ± 0.2 μM Keep at RT. This is a glutaminergic NMDA receptor antagonist and stimulates dopamine release by binding to the ion channel site. It is used in researches on Parkinson's disease, spasms, Alzheimer's disease and so on. (+)-MK 801 Maleate, 98.0+ % (HPLC) 130-17381 10 mg 136-17383 50 mg for Cellbiology 77086-22-7 Methanol Ki = 30.5 ± 1.5 nM Keep at 2-10℃. Selective antagonist of NMDA glutamate receptor. It inhibits calcium ion influx across cell membranes by binding mainly to the pore of the ion channel opened upon the ligand binding. It is known as an anti-ischemic agent. NBQX Disodium Salt, 98.0+ % (HPLC) 147-08661 10 mg for Cellbiology 479347-86-9 Water - Keep at 2-10℃. Water-soluble NBQX. NBQX is a potent and competitive AMPA/kainate receptor antagonist. NBQX, 99+ % (TLC) 7. Neurotransmitter Inhibitors 148-06751 24 10 mg for Biochemistry 118876-58-7 Acetone IC50 = 0.90 μM Keep at 2-10℃. IC50 = 2 - 18 μM Keep at -20℃. Antagonist of the AMPA/kainate receptor. Pentamidine Isethionate, 98.0+ % (HPLC) 166-25191 50 mg for Cellbiology 140-64-7 Water This substance exhibits nerve protection activity and inhibits homeostatic NO synthase in the brain. It is an antagonist to NMDA glutamate receptor. It inhibits glucose metabolism and protein synthesis in Pneumocystis carinii. for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in 71-44-3 Water, chloroform IC50 Storage Condition Summary Spermine, 95.0+ % (Titration) 198-09811 250 mg 194-09813 1g for Biochemistry IC50 = 170 μM Keep at 2-10℃. Agonist during depolarization and antagonist during hyperpolarization. (2) Inhibitors of Angiotensin Conversion Enzyme Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Ethanol - Keep at RT. Summary Benazepril Hydrochloride, 97.0+ % (HPLC) 024-14091 1g 020-14093 5g for Biochemistry 86541-74-4 ACE inhibitor used clinically as a therapeutic for hypertension. Captopril, 96.0+ % (Titration) 039-20951 1g 035-20953 5g 037-20952 25 g for Pharmacology Research 62571-86-2 Methanol, acetone, water Keep below 25℃. IC50 = 9 nM Angiotensin converting enzyme (ACE) inhibitor that blocks ACE and inhibits the pressor system while enhancing the depressor system. It is a crude drug for essential and renal hypertensions. Enalaprilat Dihydrate, 98.0+ % (HPLC) 055-06851 1g for Biochemistry 84680-54-6 Methanol IC50 = 4.8 nM Keep at RT. This is an active form of enalapril, which is an angiotensin converting enzyme (ACE) inhibitor. One of the percutaneous vasodilators. Enalapril Maleate, 98.0+ % (HPLC) 051-06711 1g 057-06713 5g for Biochemistry 76095-16-4 Methanol, ethanol IC50 = 1 - 10 nM Keep at RT. IC50 = 1.2 nM Keep at RT. It inhibits angiotensin II synthesis by inhibiting angiotensin converting enzyme. Lisinopril Dihydrate, 98.0+ % (HPLC) 128-04711 1g 124-04713 5g for Biochemistry 76547-98-3 Water It inhibits angiotensin II production by blocking angiotensin converting enzyme, and has antihypertensive effects. It is a crude drug for treating hypertension, chronic heart failure, etc. (3) Cannabinoid Receptor Antagonists Product Name Wako Cat. No. Pkg. Size Grade CAS No. for Biochemistry 149301-79-1 Soluble in IC50 Storage Condition Summary 011-18461 10 mg Ethanol IC50 = 15 μM Selective inhibitor of cellular phospholipase A2 (cPLA2) and Ca independent phospholipase A2 (iPLA2) (IC50 = 15 μM). 2+ Keep at -20℃. 7. Neurotransmitter Inhibitors AACOCF3 25 Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in for Cellbiology 183232-66-8 DMSO, DMF IC50 Storage Condition Summary AM 251, 95.0+ % (HPLC) 011-24191 2 mg 017-24193 10 mg 015-24194 50 mg IC50 = 8.9 μM Keep at -20℃. Potent CB1 receptor antagonist/inverse agonist. Ki = 7.5 nM. It is an analog of a cannabinoid receptor antagonist, SR141716A. AM 281, 97.0+ % (HPLC) 012-22161 2 mg 018-22163 10 mg for Cellbiology 202463-68-1 Methanol Keep at 2-10℃. IC50 = 6 nM Potent CB1 receptor antagonist/inverse agonist. Ki = 14 nM. It is an analog of a cannabinoid receptor antagonist, SR141716A. AM 630 019-22551 2 mg 015-22553 10 mg for Cellbiology 164178-33-0 DMSO IC50 = 6.3 μM Keep at 2-10℃. Antagonist/inverse agonist of cannabinoid receptor subtype CB2 (Ki = 31.2 nM). (4) GABA Receptor Antagonists Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in 485-49-4 Methanol, chloroform IC50 Storage Condition Summary (+)-Bicuculline, 98.0+ % (HPLC) 026-16131 50 mg 022-16133 250 mg for Cellbiology IC50 = 4.5 μM Keep at -20℃. Lactone of bixin, known for its use as a proconvulsant. It is a selective antagonist of GABA(A) receptor, a GABA receptor subtype that exists in the central and peripheral nervous systems. Because this reagent binds to GABA binding site, it competitively blocks GABA and muscimol actions. (-)-Bicuculline Methobromide 026-14291 100 mg for Biochemistry IC50 = 15 nM Keep at 2-10℃. - IC50 = 0.8 ± 0.2 μM Keep at -20℃. 124-87-8 Ethanol IC50 = 2.6 ± 0.4 μM Keep at RT. 17617-45-7 Ethanol, Chloroform IC50 = 25 ± 0.4 μM Keep at 2-10℃. 73604-30-5 Water GABAA receptor antagonist. (-)-Bicuculline Methochloride, 93.0+ % (HPLC) 026-17611 10 mg 022-17613 50 mg for Biochemistry 53552-05-9 Water-soluble methochloride salt of (+)-bicuculline Picrotoxin, 97.0+ % (HPLC) 168-17961 1g 164-17963 5g Wako 1st Grade GABAA receptor antagonist. Picrotoxinin, 95.0+ % (HPLC) 165-17351 500 mg for Biochemistry 7. Neurotransmitter Inhibitors A bitter component isolated from a plant of family Menispermaceae (Anamirta cocculus). The toxic moiety of picrotoxin (central nerve excitation agent), which blocks the Cl- channel in an allosterical manner that forms a molecular complex with GABA receptors. 26 for other products, please visit the Wako Online Catalog www.e-reagent.com (5) Serotonin-related Inhibitors Product Name Wako Cat. No. Pkg. Size CAS No. Grade Soluble in IC50 Storage Condition Summary Amitriptyline Hydrochloride, 99.0+ % (Titration) 013-12882 25 g for Biochemistry 549-18-8 Water, chloroform, 5-HT: IC50 = 39 nM ethanol NA: IC50 = 21 nM Keep at RT. Tricyclic antidepressant substance, anxiolytic substance. It inhibits reuptake of noradrenaline and serotonin in the brain and exerts an antidepressant action. Amoxapine, 98.0+ % (HPLC) 015-23631 011-23633 1g 5g for Pharmacology Research 14028-44-5 Acetic acid, glacial, chloroform, dichloroethane - Keep at RT. This is a tricyclic antidepressant. It inhibits reuptake of serotonin (5-HT) and noradrenaline in nerve terminals in the brain. Azasetron Hydrochloride, 90.0+ % (HPLC) 014-24441 50 mg 010-24443 200 mg for Biochemistry 123040-16-4 Water - 5-HT3 Receptor Antagonist Blonanserin, 98.0+ % (HPLC) 022-17451 5 mg 028-17453 50 mg for Pharmacology Research 132810-10-7 Acetonitrile, acetic Ki = 0.812 nM (5-HT2A); 0.142 nM acid, methanol, (Dopamine D2); 0.494 nM (Dopamine D3) ethanol Keep at RT. This substance binds selectively to dopamine D2 receptor and serotonin 5-HT2 receptor and exhibits antagonistic activities. DL-p-Chlorophenylalanine, 99.0+ % (Titration) 037-10741 1g 033-10743 5g 035-10742 25 g Wako Special Grade 7424-00-2 Dilute hydrochloric acid - Keep at RT. It irreversibly binds to tryptophan hydroxylase and decreases intracerebral serotonin (serotonin synthetic inhibitor). Citalopram Hydrobromide, 98.0+ % (HPLC) 031-22231 25 mg 037-22233 100 mg for Pharmacology Research 59729-32-7 Water, ethanol IC50 = 1.8 nM Keep at 2-10℃. Citalopram Hydrobromide is a selective serotonin reuptake inhibitor (SSRI). This reagent blocks the reuptake of intracerebral serotonin and exhibits antidepressive effects by increasing serotonin in the synaptic cleft. It is considered to have almost no affinity for other neurotransmitter receptors. Clomipramine Hydrochloride, 98.0+ % (volumetric analysis), 98.0+ % (HPLC) 036-21941 032-21943 1g 5g for Pharmacology Research 17321-77-6 Water, acetic acid, methanol, chloroform IC50 of 5-HT: 1.5 nM; NA: 24 nM Keep at RT. Clomipramine Hydrochloride is a derivative of imipramine and has tricyclic antidepressant effects. This reagent blocks the uptake of intracerebral serotonin (5-HT) and noradrenaline into the nerve terminal. It potently blocks serotonin uptake. Desipramine Hydrochloride, 99.0+ % (Titration); 99+ % (TLC) 044-23121 1g 040-23123 5g for Biochemistry 58-28-6 Chloroform, water, IC50 of 5-HT: 382 nM; NA: 1.26 nM ethanol Keep at RT. Tricyclic antidepressant. It binds to amine transporter and blocks reuptake of intracerebral serotonin (5-HT) and noradrenaline into the nerve terminal. It is an active metabolite of imipramine. 043-32001 1g 049-32003 5g for Pharmacology Research 1229-29-4 Water IC50 of 5-HT: 280 nM; NA: 40 nM Tricyclic antidepressant. It blocks the reuptake of serotonin and noradrenaline. It is a potent H1 histamine receptor antagonist. Keep at RT. 7. Neurotransmitter Inhibitors Doxepin Hydrochloride (mixture of isomers), 98.0+ % (HPLC) 27 Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary Duloxetine Hydrochloride, 98.0+ % (HPLC) 041-32041 10 mg 047-32043 100 mg for Pharmacology Research 136434-34-9 Methanol, DMSO IC50 of 5-HT: 6.3 nM; NA: 5.8 nM Keep at RT. Tricyclic antidepressant. It blocks the reuptake of serotonin and noradrenaline. It is a potent H1 histamine receptor antagonist. (±)-Fluoxetine Hydrochloride, 98.0+ % (HPLC) 068-04321 10 mg 064-04323 50 mg 068-04326 1g for Biochemistry 56296-78-7 Methanol, ethanol, acetonitrile, IC50 = 6.8 nM chloroform, acetone Keep below 25℃. Selective serotonin reuptake inhibitor (SSRI). It inhibits serotonin reuptake and consequently elevates serotonin concentration in synaptic gaps exhibiting antidepressive effect. Fluvoxamine Maleate 065-05171 5g 061-05173 100 g for Pharmacology Research 61718-82-9 Ethanol IC50 = 0.29 nM Keep at 2-10℃. Selective serotonin reuptake inhibitor (SSRI). It is used for treating melancholia, depression, obsessive compulsive disorder, and social anxiety disorder. Granisetron Hydrochloride, 98.0+ % (HPLC) 073-06131 5 mg 079-06133 50 mg for Pharmacology Research 107007-99-8 Water IC50 = 0.20 nM Keep at 2-10℃. IC50 of 5-HT: 28.0 nM; NA: 29.6 nM Keep at -20℃. Highly selective serotonin receptor 5-HT3 antagonist. It is an antiemetic. Milnacipran Hydrochloride, 98.0+ % (HPLC) 133-17011 25 mg 139-17013 100 mg for Pharmacology Research 101152-94-7 Water Serotonin-noradrenaline reuptake inhibitor (SNRI). It selectively binds to the reuptake site of serotonin and noradrenaline at nerve terminals thus inhibiting uptake of monoamine and increasing extracellular concentrations of serotonin and noradrenaline in the brain. Olanzapine, 98.0+ % (HPLC) 150-03071 156-03073 50 mg 500 mg for Pharmacology Research 132539-06-1 Acetonitrile Ki of 5-HT2A: 2.5 nM; 5-HT2B: 11.8 nM; 5-HT2C: 28.6 nM; 5-HT6: 2.5 nM; Dopamine D2: 11 nM; Dopamine D3: 16 nM; Dopamine D4: 27 nM; α1-adrenaline: 19 nM; Histamine H1: 7 nM Keep at RT. Olanzapine antagonizes various neuronal receptors including serotonin 5-HT2A, 2B, 2C, 5-HT6, dopamine D2, D3, D4, α1-adrenaline, histamine H1 receptors. Paroxetine Hydrochloride, 98.0+ % (HPLC) 168-24431 100 mg for Pharmacology Research 78246-49-8 Water IC50 = 0.29 nM Keep below 25℃. Potent and selective serotonin reuptake inhibitor (SSRI) in the serotonin neuron system in brain Perospirone Hydrochloride Dihydrate, 98.0+ % (HPLC) 167-25241 5 mg 163-25243 50 mg for Pharmacology Research 192052-81-6 Methanol, ethanol, 5-HT2: Ki=0.61 nM; Dopamine D2: 1.4 nM acetonitrile, water Keep at RT. It binds selectively to dopamine D2 receptor and serotonin 5-HT2 receptor and exhibits antagonistic activities. 7. Neurotransmitter Inhibitors Quetiapine Fumarate, 98.0+ % (HPLC) 28 172-00691 178-00693 1g 10 g for Pharmacology Research 111974-72-2 N,NDimethylformamide IC50 of 5-HT2: 148 nM; Dopamine D2: 329 nM; adrenaline α1: 94 nM; Histamine H1: 30 nM Keep at RT. Dibenzothiazepine compound. It inhibits dopamine D2 receptor and serotonin 5HT2 receptor. It shows affinity to a number of receptors other than dopamine D2 and serotonin 5HT2. It shows higher affinity to serotonin 5HT2 receptor than dopamine D2 receptor. for other products, please visit the Wako Online Catalog www.e-reagent.com Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition for Pharmacology Research 106266-06-2 Methanol - Keep at RT. Summary Risperidone 188-02311 50 mg 184-02313 250 mg It binds selectively to dopamine D2 receptor and serotonin 5-HT2A receptor and exhibits antagonistic activities. Sertraline Hydrochloride, 98+ % (HPLC) 193-16191 100 mg 199-16193 1g for Pharmacology Research 79559-97-0 Methanol IC50 = 0.058 μM Keep at RT. Selective serotonin reuptake inhibitor (SSRI). It exhibits antidepressant activity by the inhibition of serotonin reuptake in the brain and increase in the amount of serotonin in synaptic gaps. Trazodone Hydrochrolide, 98.0+ % (HPLC) 209-14964 500 mg for Biochemistry 25332-39-2 Water IC50 of 5-HT uptake: 580 nM; NA uptake: 11 μM Keep at 2-10℃. Triazolopyridine antidepressant, which acts more selectively on serotonin than on noradrenaline in its inhibition of monoamine reuptake and exerts antidepressant activity. It has almost no anti-cholinergic effects and hardly inhibits reuptake of noradrenalin in the heart. Venlafaxine Hydrochloride, 98.0+ % (HPLC) 227-01951 500 mg for Pharmacology Research 99300-78-4 Water Ki = 41.0 ± 9.1 μM Keep at RT. Serotonin-noradrenaline reuptake inhibitor (SNRI). It selectively binds to the reuptake site of serotonin and noradrenaline at nerve terminals thus inhibiting uptake of monoamine and increasing extracellular concentrations of serotonin and noradrenaline in the brain. (6) Dopamine Receptor Antagonists Product Name Wako Cat. No. Pkg. Size CAS No. Soluble in 129722-12-9 Benzyl alcohol, acetic acid Grade IC50 Storage Condition Summary Aripiprazole, 98.0+ % (HPLC) 017-23831 100 mg 013-23833 1g for Pharmacology Research IC50 = 37 nM (with 100 nM Dopamine) Keep at RT. Quinoline derivative antagonist of dopamine D2 receptor when dopamine is insufficient. It also acts as partial agonist of serotonin 5-HT1A receptor and dopamine D2 receptor and antagonist of serotonin 5-HT2A receptor. Bupropion Hydrochloride, 98.0+ % (HPLC) 028-17311 100 mg 024-17313 1g for Pharmacology Research 21535-47-7 Methanol IC50 of NA transporter: 1.4 μM; DA transporter: 2.8 μM Keep at RT. Noradrenaline-dopamine reuptake inhibitors (DNRIs). It inhibits the reuptake of noradrenalin and dopamine into the nerve terminals in the brain, thereby increasing the extracellular serotonin concentrations of noradrenaline and dopamin in the brain. Clozapine, 98.0+ % (HPLC) 038-22741 10 mg 034-22743 50 mg for Pharmacology Research 5786-21-0 Ethanol IC50 of D4: 9 nM; 5-HT2A: 12 nM; 5-HT2C: 8 nM Keep at RT. Subtype D4 selective dopamine receptor antagonist. It also antagonizes serotonin receptors (5-HT2A, 5-HT2C, 5-HT3, 5-HT6, 5-HT7). Haloperidol, 98.0+ % (Titration) 1g 080-04263 5g 082-04262 25 g Wako Special Grade 52-86-8 Acetic acid, glacial, chloroform - Keep at RT. Haloperidol antagonizes especially dopamines at the dopamine receptor and blocks their action. (+)-SCH23390 Hydrochloride, 98.0+ % (HPLC) 191-15531 10 mg 197-15533 50 mg for Cellbiology 125941-87-9 DMF IC50 of D1: 0.2 nM; D5: 0.3 nM Keep at 2-10℃. 7. Neurotransmitter Inhibitors 084-04261 Potent dopamine D1 receptor antagonist. It also potently agonizes 5-HT1C/2C receptors. 29 Product Name Wako Cat. No. Pkg. Size CAS No. Soluble in 15676-16-1 Acetic acid, glacial Grade IC50 Storage Condition Summary (±)-Sulpiride, 98.0+ % (Titration) 190-12061 1g 198-12062 25 g 196-12063 100 g for Biochemistry Keep at 2-10℃. D2: IC50 = 4 nM This product blocks dopamin D2 receptors, thereby increasing the extracellular dopamine levels in the brain. It exhibits little antagonist action on the receptors of monoamine such as adrenaline and serotonin. (7) Noradrenaline-related Inhibitors Product Name Wako Cat. No. Pkg. Size CAS No. Grade Soluble in IC50 Storage Condition Summary Maprotiline Hydrochloride, 98.0+ % (HPLC) 139-17091 1g 135-17093 5g for Pharmacology Research 10347-81-6 Methanol, chloroform IC50 = 8.4 nM Keep at RT. Tetracyclic antidepressant. It increases noradrenaline concentrations by inhibiting the reuptake of noradrenaline into the nerve terminals. Mianserin Hydrochloride 132-16861 138-16863 50 mg 500 mg for Pharmacology Research 21535-47-7 Methanol IC50 of α2 adrenaline receptor: 12 nM; α adrenaline receptor: 300 nM; 5-HT receptor: 22 nM Keep at RT. Tetracyclic antidepressant. It blocks presynaptic α2 adrenaline autoreceptor, thereby accelerates noradrenaline release into synaptic gaps. Acceleration of metabolic turnover of noradrenaline in the brain has also been reported. It exhibits 5-HT receptor blocking activity. Mirtazapine, 98.0+ % (HPLC) 134-16821 130-16823 10 mg 50 mg for Pharmacology Research 85650-52-8 pKi = 6.9 - 7.0 (α2); 5.2 (5-HTA1); Ethanol, methanol, 7.88 (5-HT2); 6.8, 8.1 (5-HT3); chloroform 5.5 - 5.8 (NA uptake); <5.0 (5-HT uptake) Keep at RT. Noradrenergic and specific serotonergic antidepressant. Mirtazapine acts as an antagonist on presynaptic α2-adrenergic autoreceptors and heteroreceptors and enhances noradrenaline and serotonin (5-HT) releases and adrenergic and serotonergic neurotransmission in the brain. It also blocks 5-HT2 and 5-HT3 receptors and selectively activates 5-HT1A receptors. (8) Alzheimer's Disease Research Product Name Wako Cat. No. Pkg. Size CAS No. Soluble in IC50 Storage Condition 290315-45-6 - - Keep at -20℃. Grade Summary BMS 299897, 97.0+ % (HPLC) 021-17781 5 mg 027-17783 25 mg for Cellbiology Potent γ-secretase inhibitor that inhibits the formation of the amyloids Aβ40 and Aβ42 in vitro. It is also known not to inhibit Notch signaling. It has oral activity. DAPT, 97.0+ % (HPLC) 045-30981 5 mg 041-30983 25 mg for Cellbiology 208255-80-5 Methanol - Keep at -20℃. Water (1 mg/mL) - Keep at 2-10℃. 7. Neurotransmitter Inhibitors γ-secretase inhibitor. Donepezil Hudrochloride, 90.0+ % (HPLC) 045-32321 50 mg 041-32323 250 mg for Biochemistry 120011-70-3 Reversible acetylcholinesterase (AChE) inhibitor. Donepezil-induced downregulation of AChE leads to increased levels of acetylcholine in the brain, which in turn stimulates cholinergic nerve system in the brain. L-685, 458, 98.0+ % (HPLC) 121-06141 1 mg for Cellbnioloty 292632-98-5 DMSO (>10 mg/mL) - Keep at -20℃. Potent and selective γ-secretase inhibitor. It also inhibits with equal potency to Aβ40 and Aβ42 peptides. 30 for other products, please visit the Wako Online Catalog www.e-reagent.com Index Product Name PAGE A A-83-01 ················································· 1 AACOCF3 ············································ 25 17-AAG ·················································· 1 AG 1296 ················································ 1 AG 1478 ················································ 1 AG 490 ·················································· 1 ω-Agatoxin IVA ···································· 15 ω-Agatoxin TK ····································· 15 Agelenin ··············································· 15 Alendronate Sodium Salt Trihydrate ···· 14 ALK5 Inhibitor ········································ 1 AM 251 ················································ 26 AM 281 ················································ 26 AM 630 ················································ 26 AMG 9810 ··········································· 19 DL-2-Amino-4-phosphonobutyric Acid ··· 23 L-2-Amino-4-phosphonobutyric Acid ··· 23 D(-)-2-Amino-5-phosphonovaleric Acid ··· 23 DL-2-Amino-5-phosphonovaleric Acid ··· 23 Aminogenistein ······································ 1 Amitriptyline Hydrochloride ················· 27 Amlodipine ·········································· 16 Amoxapine ·········································· 27 Andrographolide ·································· 22 AP 18 ··················································· 20 Apamin ················································ 17 2-APB ·················································· 20 APETx2 ················································ 21 Apigenin ················································ 1 Aripiprazole ········································· 29 AS 604850 ············································· 1 AS 605240 ············································· 2 ATM Kinase Inhibitor ····························· 2 Azasetron Hydrochloride ····················· 27 B BAY 11-7085 ······································· 22 BCTC ··················································· 20 Benazepril Hydrochloride ···················· 25 (+)-Bicuculline ······································ 26 (-)-Bicuculline Methobromide ·············· 26 (-)-Bicuculline Methochloride ·············· 26 Bio ························································· 2 (-)-Blebbistatin ····································· 14 Blonanserin ·········································· 27 BMS 299897 ········································ 30 6-Bromoindirubin-3'-oxime ··················· 2 Bupropion Hydrochloride ···················· 29 2,3-Butanedione Oxime ······················ 16 Butein ···················································· 2 C Calcicludine ········································· 16 Calciseptine ········································· 16 Calpain Inhibitor 2 ······························· 14 Calphostin C ·········································· 2 Calyculin A ··········································· 12 Cantharidin ·········································· 12 Capsazepine ········································ 20 Captopril ·············································· 25 Carbonyl Cyanide m-Chlorophenylhydrazone ················· 2 Charybdotoxin ····································· 17 DL-p-Chlorophenylalanine ·················· 27 8-(4-Chlorophenylthio)adenosine 3,5-(Cyclic) monophosphate Sodium Salt ················· 22 Chlorotoxin ·········································· 21 Chlorpromazine Hydrochloride ············ 14 Cinnarizine ··········································· 16 Citalopram Hydrobromide ··················· 27 CKI-7 Dihydrochloride ··························· 2 Clomipramine Hydrochloride ··············· 27 Clotrimazole ········································ 19 Clozapine ············································· 29 Compound 15e ······································ 2 Compound 401 ····································· 2 α-Conotoxin G1 ··································· 21 μ-Conotoxin G3B ································ 19 μ-Conotoxin GS ·································· 19 ω-Conotoxin GVIA ······························· 16 α-Conotoxin ImI ··································· 21 α-Conotoxin M1 ·································· 21 ω-Conotoxin MVIIA ······························ 16 ω-Conotoxin MVIIC ····························· 16 α-Conotoxin S1 ··································· 21 μ-Conotoxin SIIIA ································ 19 ω-Conotoxin SVIB ······························· 16 (R)-CPP ················································ 23 Curcumin ············································· 22 Cyclopiazonic Acid ······························ 14 Cyclosporin A ······································ 12 E-64d ··················································· Enalaprilat Dihydrate ··························· Enalapril Maleate ································· Evans Blue ··········································· 14 25 25 24 F Felbamate ············································ (±)-Fluoxetine Hydrochloride ·············· Fluphenazine Dimaleate ······················ Fluvoxamine Maleate ·························· Fostriecin Sodium Salt ························ 24 28 14 28 12 G Geldanamycin ······································· 3 Genistein ··············································· 3 Genistin ················································· 3 GF 109203X ··········································· 3 Glibenclamide ······································ 18 Gö 6983 ················································· 3 Granisetron Hydrochloride ·················· 28 GSK-3 Inhibitor IX ································· 2 GSK 269962A ········································ 3 GSK 429286A ········································ 4 GsMTx-4 ·············································· 21 Guangxitoxin-1E ·································· 18 H H-1152 Dihydrochloride ························ 4 Haloperidol ·········································· 29 HC-030031 ·········································· 20 Herbimycin A ········································· 4 Huwentoxin-IV ····································· 19 Hypericin ··············································· 4 D I D-AP5 ·················································· 23 DL-AP5 ················································ 23 DAPT ··················································· 30 Deguelin ················································ 2 Dendrotoxin 1 ······································ 18 Desipramine Hydrochloride ················· 27 Dextromethorphan Hydrobromide Monohydrate ······································ 23 Diazoxide ············································· 23 Dibucaine Hydrochloride ······················· 3 Diltiazem Hydrochloride ······················ 16 Disodium β-Glycerophosphate Pentahydrate ····································· 12 2,5-Di-t-butylhydroquinone ················· 14 DL-AP7 ················································ 23 DNQX ·················································· 23 Donepezil Hudrochloride ····················· 30 Dorsomorphin ········································ 3 Dorsomorphin Dihydrochloride ············· 3 Doxepin Hydrochloride ························ 27 Duloxetine Hydrochloride ···················· 28 Iberiotoxin ············································ 18 IPA-3 ······················································ 4 Isotetrandrine ······································ 22 E E-4031 n-Hydrate ································ 18 J Joro Spider Toxin JSTX-3 ···················· 24 K K-252a ··················································· 4 K-252b ··················································· 4 Kaliotoxin (1-37) ·································· 18 Kenpaullone ··········································· 4 Ki 8751 ·················································· 4 KN-62 ···················································· 5 KN-93 ···················································· 5 KN-93, Water-Soluble ··························· 5 KT 5720 ················································· 5 KT 5823 ················································· 5 KU 0063794 ··········································· 5 Kurtoxin ··············································· 17 L L-685, 458 ··········································· 30 LDN 193189 Hydrochloride ··················· 5 31 Index Product Name PAGE Levamisole Hydrochloride ··················· 12 Lisinopril Dihydrate ······························ 25 Loperamide Hydrochloride ·················· 24 LY-83583 ·············································· 22 LY 294002 ·············································· 5 Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-AlaPhe-Asp-Ala-Tyr ·································· 6 M Maprotiline Hydrochloride ··················· 30 Margatoxin ··········································· 18 Mastoparan ········································· 15 MCD-Peptide ······································ 18 (+)-MCPG ············································ 24 Memantine Hydrochloride ··················· 24 3-Methyladenine ···································· 6 MG-132 ··············································· 15 MgTX ··················································· 18 Mianserin Hydrochloride ····················· 30 Milnacipran Hydrochloride ·················· 28 Mirtazapine ·········································· 30 (+)-MK 801 Maleate ····························· 24 N NBQX ··················································· 24 NBQX Disodium Salt ··························· 24 Nicardipine Hydrochloride ··················· 17 Nitrendipine ········································· 17 NS2028 ················································ 22 NSC 693868 ·········································· 6 NU 7026 ················································ 6 NU 7441 ················································ 6 O ODQ ····················································· 22 Olanzapine ··········································· 28 Olomoucine ··········································· 6 Olvanil ·················································· 20 Omeprazole ········································· 19 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin1-one ················································· 22 P Paroxetine Hydrochloride ···················· 28 PD-98059 ·············································· 6 PD 173074 ············································· 6 PD 184352 ············································· 6 PD 0325901 ··········································· 7 Pentamidine Isethionate ······················ 24 Pentoxifylline ······································· 22 Perospirone Hydrochloride Dihydrate ··· 28 Phloretin ················································ 7 Phosphatase Inhibitor Cocktail Solution I ··· 13 Phosphatase Inhibitor Cocktail Solution II ··· 13 PI-103 ···················································· 7 Piceatannol ············································ 7 Picrotoxin ············································ 26 Picrotoxinin ·········································· 26 PIK-75 Hydrochloride ···························· 7 32 PKC 412 ················································ 7 PLTX-II ················································· 17 PP 2 ······················································ 7 PP 3 ······················································ 7 PP 242 ··················································· 7 Protease Inhibitor Cocktail Set I ·········· 13 Protease Inhibitor Cocktail Set III ········ 13 Protease Inhibitor Cocktail Set IV ········ 13 Protease Inhibitor Cocktail Set V ········· 13 Protease Inhibitor Cocktail Set VI ········ 13 Protease Inhibitor Cocktail Set VII ······· 13 ProTx-1 ················································ 17 ProTx-II ················································ 19 Psalmotoxin 1 ······································ 21 Purotoxin-1 ·········································· 21 Suramin Sodium ·································· 15 T Tamoxifen Citrate ································ 10 Tautomycin ·········································· 12 Tertiapin ··············································· 18 TGF-β R I Kinase Inhibitor IV ················· 1 Thapsigargin ········································ 15 Tityustoxin Kα ······································ 19 Trazodone Hydrochrolide ···················· 29 Triciribine ············································· 10 TWS 119 ·············································· 10 Tyrphostin A25 ····································· 10 U U 0126 ················································· 11 Q Quercetin Dihydrate ······························ 8 Quetiapine Fumarate ··························· 28 Quinacrine Dihydrochloride Dihydrate 15 V Venlafaxine Hydrochloride ··················· 29 Verapamil Hydrochloride ····················· 17 R W Rac1 Inhibitor ········································ 8 Radicicol ················································ 8 Rapamycin ············································ 8 RG-14620 ·············································· 8 Risperidone ········································· 29 RK-682 ················································ 12 RN-1747 ·············································· 20 Ro 31-8220 Methanesulfonate ·············· 8 Rolipram ·············································· 23 Roscovitine ············································ 8 Ruthenium Red ···································· 20 Ryanodine ··········································· 17 W-5 Hydrochloride ······························ 11 W-7 Hydrochloride ······························ 11 (+)-Wortmannin ···································· 11 Y Y-27632 ··············································· 11 5 mmol/L Y-27632 Solution ················· 11 S SB 202190 ············································· 8 SB 203580 ············································· 9 SB 203580 Hydrochloride ····················· 9 SB-366791 ·········································· 20 SB 415286 ············································· 9 SB 431542 ············································· 9 (+)-SCH23390 Hydrochloride ·············· 29 Scyllatoxin ··········································· 18 Sertraline Hydrochloride ······················ 29 SNX-482 ·············································· 17 SP 600125 ············································· 9 Spermine ············································· 25 D-erythro-Sphingosine ·························· 9 SR 3677 Hydrochloride ························· 9 Staurosporine ········································ 9 Stellettamide A Trifluoroacetate ············ 9 Stichodactyla Toxin ····························· 18 SU 4312 ··············································· 10 SU 5402 ··············································· 10 SU 5416 ··············································· 10 SU 6668 ··············································· 10 SU 11274 ············································· 10 (±)-Sulpiride ········································ 30 for other products, please visit the Wako Online Catalog www.e-reagent.com