TCS PIM-1 1

半岛bd体育手机客户端名称：

491871-58-0
TCS PIM-1 1
SC 20433

半岛bd体育手机客户端介绍：

基本信息

分子式	C₁₈H₁₁BrN₂O₂
分子量	367.20
存储条件	Freezer -20℃

半岛bd体育手机客户端描述

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.