JSH-150

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Chemical Structure| 2247481-21-4 同义名 : -
CAS号 : 2247481-21-4
货号 : A1275146
分子式 : C24H33ClN6O2S
纯度 : 99%+
分子量 : 505.076
MDL号 : MFCD31807311
存储条件：

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(207.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.90mL

1.98mL

0.99mL

19.80mL

3.96mL

1.98mL
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