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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-JSH-150
JSH-150

Chemical Structure : JSH-150

CAS No.: 2247481-21-4

JSH-150 (JSH150;JSH 150)

货号: PC-35688Not For Human Use, Lab Use Only.

JSH-150 (JSH150) is a potent, highly selective inhibitor of CDK9 kinase with IC50 of 1 nM in the biochemical assays, displays 300-10000-fold selectivity over other CDK kinase family members (CDK7 IC50=1.72 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JSH-150 (JSH150) is a potent, highly selective inhibitor of CDK9 kinase with IC50 of 1 nM in the biochemical assays, displays 300-10000-fold selectivity over other CDK kinase family members (CDK7 IC50=1.72 uM).
JSH-150 also exhibits high selectivity over other 468 kinases/mutants (KINOMEscan S score(1) = 0.01).
JSH-150 displays potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines, dose-dependently inhibits the phosphorylation of RNA Pol II, suppresses the expression of MCL-1 and c-Myc, arreststhe cell cycle and induces the apoptosis in the leukemia cells.
JSH-150 completely suppresses the tumor progression in MV4-11 cell-inoculated xenograft mouse model (10 mg/kg).

物理化学性质&存储条件

分子量 505.078
分子式 C24H33ClN6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(((4-(5-Chloro-2-(((1r,4r)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile

参考文献

1. Wang B, et al. Eur J Med Chem. 2018 Oct 5;158:896-916.

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