• K252a is a kinase inhibitor that inhibits PKA (Ki = 18 nM), PKC (Ki = 25 nM), and PKG (Ki = 20 nM). Kase, H., et al. "K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases." Biochem. Biophys. Res. Commun. 142: 436-440 (1987).
• Potently inhibits CaMK (Ki = 1.8 nM), competitively with ATP and noncompetitively with the substrate. Hashimoto, Y., et al. "Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926." Biochem. Biophys. Res. Commun. 181: 423-429 (1991).
• Potently inhibits phosphorylase kinase (IC50 = 1.7 nM), with 300-fold selectivity for this enzyme over protein kinase C. Elliott, L.H., et al. "K252a is a potent and selective inhibitor of phosphorylase kinase." Biochem. Biophys. Res. Commun. 171: 148-154 (1990).
• Potent inhibitor of the tyrosine phosphorylation of p140prototrk; K252a also has a direct effect on the p140prototrk tyrosine kinase. Berg, M.M., et al. "K-252a Inhibits Nerve Growth Factor-induced trk Proto-oncogene Tyrosine Phosphorylation and Kinase Activity." J. Biol. Chem. 267: 13-16 (1992).
• Potent inhibitor of pp42/44 MAP kinase in vitro and in vivo. Lloyd, E.D. and Wooten, M.W. "pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells." J. Neurochem. 59: 1099-1109 (1992).
• K252a apparently induces apoptosis by suppressing phosphorylation of Rb, upregulating p21, and inhibiting Cdc2 and Cdc25c activity. Mohri, T., et al. "K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c." Cancer Invest. 17: 391-395 (1999).
• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
• We note that one of our competitors, AG Scientific, as of February 11, 2014, is claiming 99.86% purity for its K252a. This claim is not credible in general chemical terms for this complex organic compound, nor in terms of the sensitivity and reproducibility of generally utilized analytical techniques.

Related Terms:

[K-252a]
M.W. 467.47
C27H21N3O5
[97161-97-2]

Storage

Store at or below -20 ºC

Solubility

Soluble in DMSO at 100 mg/mL; poorly soluble in ethanol

Disposal

A

LC Laboratories 公司提供信号转导，调节蛋白亚细胞定位试剂（抗生素）产品蛋白抑制剂产品。LC Laboratories（LC Labs）公司成立于1980年，一直专注于信号转导，肿瘤以及其他临床前试剂的研究和生产，主要提供抗癌物质、酶抑制剂、激活剂和离子通道试剂。LC Labs公司不但拥有大规模的制备液相色谱纯化能力，也开发和优化了大量的具有自主知识产权的低成本高纯度生成方法，其生产的小分子试剂纯度高、价格低和销量大。1980年，LC Labs是PMA（佛波醇12-豆蔻酸 13醋酸；TPA）的全球主要生产商，36年来的销售量超过150,000瓶；1989年为研究试剂市场提供第一个纯度高价格低的毒萝卜素；1990年提供第一个纯度高价格低的冈田酸；1991年提供第一个纯度高价格低的花萼海绵诱癌素A，并且持续是这种广泛使用的磷酸酶抑制剂的全球主要生产商；1995年提供第一个异构体级别纯度的低价格Gö 6976；1996年提供第一个纯度高价格低的罗霉素A1；2002年提供第一个纯度高价格低的雷帕霉素（抗真菌抗生素）；同年，提供第一个纯度高、价格低的FK-506；2003年提供第一个纯度高价格低的来普霉素B；2004年提供第一个纯度高价格低的星孢菌素；同年，提供第一个纯度高价格低的环巴胺；2007年，LC Labs公司为临床前肿瘤相关研究引入第一组纯度高价格低的常用蛋白激酶抑制剂。