JSH-150 is a potent CDK9 inhibitor. JSH-150 exhibited an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieved around 300-10000-fold selectivity over other CDK kinase family members. In addition, it also displayed high selectivity over other 468 kinases/mutants (KINOMEscan S score(1) = 0.01). JSH-150displayed potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines. It 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.
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BMS-265246; LDC000067; Ribociclib; SU9516; Purvalanol A; Alvocidib; AZD-5597; Kenpaullone; ON123300; BS-181; Riviciclib