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JSH-150

JSH-150
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Purity:100%
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JSH-150

Catalog No. T8484Cas No. 2247481-21-4
JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$89In Stock
10 mg$156In Stock
25 mg$347In Stock
50 mg$538In Stock
100 mg$651In Stock
500 mg$1,390In Stock
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Product Introduction

Bioactivity
Description
JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).
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.
Chemical Properties
Molecular Weight505.08
FormulaC24H33ClN6O2S
Cas No.2247481-21-4
Storage & Solubility Information
Storagekeep away from direct sunlight,store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 55 mg/mL (108.89 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9799 mL9.8994 mL19.7988 mL98.9942 mL
5 mM0.3960 mL1.9799 mL3.9598 mL19.7988 mL
10 mM0.1980 mL0.9899 mL1.9799 mL9.8994 mL
20 mM0.0990 mL0.4950 mL0.9899 mL4.9497 mL
50 mM0.0396 mL0.1980 mL0.3960 mL1.9799 mL
100 mM0.0198 mL0.0990 mL0.1980 mL0.9899 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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