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1. Kinase Inhibitors 1. Kinase Inhibitors 1. Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary A-83-01 【 TGF-β R I Kinase Inhibitor IV】 018-22521 2 mg for Cellbiology 909910-43-6 DMSO - Keep at -20℃. 014-22523 10 mg <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) IC of Dephosphorylation of EGF DMSO, DMF, 50 013-17181 5 mg for Biochemistry 134036-52-5 receptor tyrosine kinase: 1.2 μmol; Keep at -20℃. methanol EGF dependent cell proliferation: 6 μmol <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 EGF- dependent 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 for Biochemistry 520-36-5 Methanol - Keep at 2-10℃. 012-18913 50 mg <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) IC50 of PI3Kα: 4.5 μM; PI3Kγ: 250 nM; 015-23131 5 mg for Cellbiology 648449-76-7 DMSO Keep at 2 - 10℃ PI3Kβ, PI3Kδ: 250 nM <Protein kinase inhibitor> Thiazolidine-dione compound, which is a potent, cell permeable and ATP-competitive inhibitor of PI3K γ. It exhibits highly selectivity. 1 Product Name Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary AS 605240, 95.0+ % (HPLC) IC50 of PI3Kα: 60 nM; PI3Kγ: 270 nM; 012-23141 5 mg for Cellbiology 648450-29-7 DMSO Keep at 2 - 10℃ 1. Kinase Inhibitors 1. PI3Kβ: 8 nM; PI3Kδ: 300 nM <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 IC50 of PKC: 50 nM; HeLa S3: 0.23 μg/mL; for Cellbiology 121263-19-2 DMSO, DMF Keep at 2-10℃. 034-15131 100 μg MCF-7: 0.18 μg/mL <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 for Biochemistry 99534-03-9 Ethanol, acetone - Keep at -20℃. 038-16991 1 g <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 - Keep at -20℃. <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) IC50 of PI3Kα: 2 nM; PI3Kβ: 16 nM; 031-21491 5 mg for Cellbiology 371943-05-4 Ethanol Keep at 2 - 10℃ PI3Kγ: 660 nM; PI3KC2β: 220 nM <Protein kinase inhibitor> Permeable morpholino pyrimidine compound. A highly selective PI3Kα inhibitor. Compound 401, 98.0+ % (HPLC) 033-21951 1 mg IC50 of DNA-PK: 0.28 μM; mTOR: 5.3 μM; for Cellbiology 168425-64-7 Methanol Keep at -20℃. 039-21953 5 mg ATM, ATR ＞ 100 μM <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 nhibiti mTOR- dependent proliferation and induce apoptosis in TSC1-/- mouse embryo fibroblasts. Deguelin Acetone, 047-29211 5 mg for Cellbiology 522-17-8 dichloromethane, - Keep at 2-10℃. acetonitrile, DMSO <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 1. Kinase Inhibitors 1. Wako Cat. No. Pkg. Size Grade CAS No. Soluble in IC50 Storage Condition Summary Dibucaine Hydrochloride, 98.0+ % (after drying)(Titration) Water, glacial acetic 049-20011 1 g for Biochemistry 61-12-1 acid, ethanol, acetone - Keep at RT. and chloroform. <Protein kinase inhibitor> Lipophilic PKC inhibitor. Inhibits Na+ and K+-ATPase activities, too. Dorsomorphin, 99.6% (HPLC, the initiall lot) 045-31221 1 mg for Cellbiology 866405-64-3 Methanol - Keep at 2 - 10℃ 041-31223 5 mg <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 for Cellbiology 1219168-18-9 Water - Keep at 2 - 10℃ 043-31803 5 mg <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 for Cellbiology 446-72-0 Ethanol - Keep at -20℃. 079-05533 100 mg <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 for Biochemistry 529-59-9 Hot methanol - Keep at 2-10℃. 076-04683 100 mg <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 IC50 of PKCα: 7 nM; PKCβ: 7 nM; PKCγ: 6 nM; 070-05801 1 mg for Cellbiology 133053-19-7 DMSO Keep at -20℃. PKCδ: 10 nM; PKCζ: 60 nM; PKCμ: 20μM <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.
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  • Family, Is a Potent Blocker of High-Threshold Ca2+ Channels with A

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    Proc. Nat!. Acad. Sci. USA Vol. 91, pp. 878-882, February 1994 Cell Biology Calcicludine, a venom peptide of the Kunitz-type protease inhibitor family, is a potent blocker of high-threshold Ca2+ channels with a high affinity for L-type channels in cerebellar granule neurons (tolns/AIZheImer dsase/n inhibitor) HUGUES SCHWEITZ, CATHERINE HEURTEAUX, PATRICK BoIs*, DANIELLE MOINIER, GEORGES ROMEY, AND MICHEL LAZDUNSKIt Institut de Pharmacologie Mol6culaire et Cellulaire, 660 Route des Lucioles, Sophia Antipolis, 06560 Valbonne, France Communicated by JosefFried, October 8, 1993 ABSTRACT Calcicludine (CaC) is a 60-amino acid poly- acid and chromatographed onto a Sephadex G50 column. The peptide from the venom of Dendroaspis angusticeps. It Is peptidic fraction was directly loaded onto a TSK (Toyosoda, structually homologous to the Kunitz-type protease Inhibitor, Japan) SP 5PW (21.5 x 150 mm) column equilibrated with 1% to dendrotoxins, which block K+ c , and to the protease acetic acid. Peptide fractions were then eluted (Fig. 1 Top), inhibItor domain of the amyloid P protein that accumultes in with a linear gradient from 1% acetic acid to 1 M ammonium Alzbeimer disease. Voltage-lamp experiments on a variety of acetate at a flow rate of 8 ml/min. The fractions obtained excitable cells have shown that CaC specificaly blocks most of the hih-threshold Ca2+ che (L-, N-, or P-type) in the (horizontal bars) were designated A-R. Fraction Q was 10-100 nM range. Particularly high densities of specific 125I- lyophilized, redissolved in 1 ml of 0.5% trifluoroacetic acid abeled CaC binding sites were found in the olfactory bulb, in plus 0.9%6 triethylamine in water, and loaded on a Lichrosorb the molecular layer ofthe dentate gyrus and the stratum oriens RP18 7-ikm (250 x 10 mm) column (Merck, Darmstadt, ofCA3 field in the hippocanal formation, and in the granular Germany) and eluted (Fig.