JSH-150

Research use only, not for human use.

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 (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); also exhibits high selectivity over other 468 kinases/mutants (KINOMEscan S score(1)=0.01); 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; completely suppresses the tumor progression in MV4-11 cell-inoculated xenograft mouse model (10 mg/kg).

JSH150;JSH 150

Angiogenesis

CDK

CDK

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——

2247481-21-4

505.08

C24H33ClN6O2S

>98% (HPLC)

——

COCCNC1CC[C@H](NC2=NC=C(Cl)C(C3=CSC(NCC4(C#N)CCOCC4)=N3)=C2)CC1

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

(-20℃)

With Ice Pack

≥ 2 years