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TCS PIM-1 1

品牌
J&K
CAS
491871-58-0
货号
2286711
规格纯度
97%, 是ATP竞争性Pim-1激酶抑制剂, IC50为50nM, 比对Pim-2和MEK1/MEK2的抑制性较高
价格
954 *本价格含增值税费
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半岛bd体育手机客户端 名称:
491871-58-0
TCS PIM-1 1
SC 20433
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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.

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