keep away from direct sunlight,store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 7,000 | |||
5 mg | 在庫あり | ¥ 20,500 | |||
10 mg | 在庫あり | ¥ 36,000 | |||
25 mg | 在庫あり | ¥ 80,000 | |||
50 mg | 在庫あり | ¥ 123,500 | |||
100 mg | 在庫あり | ¥ 149,500 | |||
500 mg | 在庫あり | ¥ 319,000 |
説明 | JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM). |
ターゲット&IC50 | CDK14-CyclinY:1.68 μM, CDK2-CyclinA:2.86 μM, CDK5-p25:4.64 μM, CDK16-CyclinY:292 nM, CDK7-CyclinH-MNAT1:1.72 μM, CDK9-CyclinT1:1 nM, CDK1-CyclinB:1.34 μM |
In vitro | A highly selective inhibitor compound 40 (JSH-150), which 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).Compound 40 displayed 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. |
In vivo | In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of 40 could almost completely suppress the tumor progression.?The high selectivity and good in vivo PK/PD profile suggested that 40 would be a good pharmacological tool to study CDK9-mediated physiology and pathology as well as a potential drug candidate for leukemia and other cancers. |
分子量 | 505.08 |
分子式 | C24H33ClN6O2S |
CAS No. | 2247481-21-4 |
keep away from direct sunlight,store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16 mg/mL (31.68 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
JSH-150 2247481-21-4 Cell Cycle/Checkpoint CDK inhibit Cyclin dependent kinase Inhibitor JSH 150 JSH150 inhibitor