JSH-150
规格
| Cas Number | 2247481-21-4 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg 或 2mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (197.98 mM); Water: 100 mg/mL (197.98 mM); Ethanol: 100 mg/mL (197.98 mM); |
| 简短描述 | CDK9 选择性抑制剂 |
| 英文简短描述 | CDK9 Selective Inhibitors |
| 过滤标签 | CDK,Cell Cycle/DNA Damage |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | JSH-150 是 CDK9 的高选择性强效抑制剂，IC50 为 1 nM。 |
| 英文描述 |
Information JSH-150 is a highly selective and potent inhibitor ofCDK9with IC50 of 1 nM. Targets CDK9 (Cell-free assay) 1 nM 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. 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. Cell Research(from reference) Cell lines：MV4-11, HL-60 and MEC-1 cells Concentrations：serially diluted/various concentrations Incubation Time：2 h |