|4-(((4-(5-氯-2-((反式-4-((2-甲氧基乙基)氨基)环己基)氨基)吡啶-4-基)噻唑-2-基)氨基)甲基)四氢-2H-吡喃-4-甲腈|CsnPharm

CAS No.: 2247481-21-4

JSH-150 Catalog No. CSN26115

JSH-150 is a highly selective CDK9 kinase inhibitor with IC50 value of 1nM. It dose-dependently inhibited the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrested the cell cycle and induced the apoptosis in the leukemia cells.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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技术信息

生物活性

描述Cyclin-dependent kinases (CDKs) are a class of serine/threonine protein kinase which play critical roles in the regulation of cell cycle or/and transcription. JSH-150 is a potent, highly selective inhibitor of CDK9 with an IC₅₀ value of 1 nM which exhibits around 300-10000-fold selectivity over other CDK kinase family members. JSH-150 displayed potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines. Further, JSH-150 could dose-dependently inhibit the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrest the cell cycle and induce the apoptosis in the leukemia cells. In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of JSH-150 could almost completely suppress the tumor progression^[1].
作用机制JSH-150 forms two hydrogen bonds in the hinge binding area with Cys106 of CDK9^[1].
参考文献

[1] Wang B, et al. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. Eur J Med Chem. 2018 Oct 5;158:896-916

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9799 mL
- 9.8995 mL
- 19.7990 mL
- 5 mM
- 0.3960 mL
- 1.9799 mL
- 3.9598 mL
- 10 mM
- 0.1980 mL
- 0.9900 mL
- 1.9799 mL

技术信息

CAS号

2247481-21-4

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H33ClN6O2S

运输

蓝冰

分子量

505.08

别名

溶解度

DMSO	100.0 mg/mL (198.0 mM)
Ethanol	100.0 mg/mL (198.0 mM)

动物实验配方

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