Description | JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM. | ||
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Targets |
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In vitro | JSH-150 exhibits an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieves around 300-10000-fold selectivity over other CDK kinase family members. In addition, it also displays high selectivity over other 468 kinases/mutants. JSH-150 displays potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines. It can 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.[1] | ||
In vivo | In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of JSH-150 can almost completely suppress the tumor progression. The high selectivity and good in vivo PK/PD profile suggests that JSH-150 will be a good pharmacological tool to study CDK9-mediated physiology and pathology as well as a potential drug candidate for leukemia and other cancers.[1] |
Selleck Chemicals提供了超过120,000种用于细胞信号通路研究的抑制剂。我们积极跟踪最新科学,因此我们的客户可以依靠我们成为最新抑制剂的领先供应商。
Selleck的生物活性化合物库由8,000多个具有经过验证的生物学和药理活性的小分子组成。这些分子的安全性和有效性已通过临床前和临床研究证明,其中许多是FDA批准的化合物。