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Calyculin A

(Synonyms: 蛋白磷酸酯酶抑制剂,(-)-Calyculin A) 目录号 : GC18106

Potent inhibitor of PP1 and PP2A

Calyculin A Chemical Structure

Cas No.:101932-71-2

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10μg
¥1,932.00
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50μg
¥3,850.00
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产品描述

Calyculin A is a natural, cell-permeable inhibitor of the serine-threonine protein phosphatases (PP) PP1 and PP2A (IC50s = 0.3-0.7 and 0.5-1 nM, respectively).[1],[2],[3] It is without significant effect against PP2B, PP2C, and PP4.[2] Through its effects on PP1 and PP2A, calyculin A has been shown to either promote or inhibit cancer cell growth in tumor cell lines and animal models.[4],[5]

Reference:
[1]. Ishihara, H., Martin, B.L., Brautigan, D.L., et al. Calyculin A and okadaic acid: Inhibitors of protein phosphatase activity. Biochem. Biophys. Res. Commun. 159(3), 871-877 (1989).
[2]. McCluskey, A., Sim, A.T.R., and Sakoff, J.A. Serine-threonine protein phosphatase inhibitors: Development of potential therapeutic strategies. Journal of Medicinal Chemistry 45(6), 1151-1175 (2002).
[3]. Lindvall, M.K., Pihko, P.M., and Kosikinen, A.M.P. The binding mode of calyculin A to protein phosphatase-1. A novel spiroketal vector model. J. Biol. Chem. 272(37), (1997).
[4]. Fujiki, H., Suganuma, M., Yoshizawa, S., et al. Mechanisms of action of okadaic acid class tumor promoters on mouse skin. Environ. Health Perspect. 93, 211-214 (1991).
[5]. Zheng, Y.G., Wu, J., Chen, Z., et al. Chemical regulation of epigenetic modifications: Opportunities for new cancer therapy. Medicinal Research Reviews 28(5), 645-687 (2008).

Chemical Properties

Cas No. 101932-71-2 SDF
别名 蛋白磷酸酯酶抑制剂,(-)-Calyculin A
化学名 N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-oxazoly]butyl
Canonical SMILES CC1C(CC2(C(C(C(O2)C(CC(C(C)C(C(C)C=C(C)C(=CC=CC(=CC#N)C)C)O)O)OC)OP(=O)(O)O)(C)C)OC1CC=CC3=COC(=N3)C(C)CCNC(=O)C(C(C(COC)N(C)C)O)O)O
分子式 C50H81N4O15P 分子量 1009.18
溶解度 DMSO: Soluble,Ethanol: Soluble 储存条件 Store at -20°C, protect from light
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1 mM 0.9909 mL 4.9545 mL 9.909 mL
5 mM 0.1982 mL 0.9909 mL 1.9818 mL
10 mM 0.0991 mL 0.4955 mL 0.9909 mL
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