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推荐产品
基本信息
英文别名SC 20433 | |
中文别名SC 20433 |
安全信息
存储条件Freezer -20℃ |
化学和物理性质
产品描述
产品描述
TCS PIM-1 1 (SC 204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM). IC50 value: 50 nM [1] Target: Pim-1 TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.
靶点（IC50 & Targe）
Pim1
参考文献
[1]. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.
[2]. Shen Y, et al. Pim-1 inhibitor attenuates trinitrobenzene sulphonic acid induced colitis in the mice. Clin Res Hepatol Gastroenterol. 2018 Sep;42(4):382-386.
