JSH-150 - 10mM in DMSO, high purity , CAS No.2247481-21-4

Item Number

J422703

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

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