Calyculin A
(Synonyms: 蛋白磷酸酯酶抑制剂,(-)-Calyculin A) 目录号 : GC18106Potent inhibitor of PP1 and PP2A
Cas No.:101932-71-2
Sample solution is provided at 25 µL, 10mM.
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).
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet