| 产品描述： | CDK9 选择性抑制剂;CDK9 Selective Inhibitors;;InformationJSH-150 is a highly selective and potent inhibitor ofCDK9with IC50 of 1 nM.TargetsCDK9 (Cell-free assay) 1 nMIn vitroJSH-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.In vivoIn 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.Cell Research(from reference)Cell lines：MV4-11, HL-60 and MEC-1 cells Concentrations：serially diluted/various concentrations Incubation Time：2 h |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京