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JSH-150

Catalog No. T8484 CAS 2247481-21-4

JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).

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JSH-150, CAS 2247481-21-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 91.00
10 mg	In stock	$ 157.00
25 mg	In stock	$ 349.00
50 mg	In stock	$ 539.00
100 mg	In stock	$ 651.00

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Purity: 100%

Purity: 99.96%

Biological Description

Chemical Properties

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Description	JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).
Targets&IC50	CDK1-CyclinB:1.34 μM, CDK9-CyclinT1:1 nM, CDK7-CyclinH-MNAT1:1.72 μM, CDK16-CyclinY:292 nM, CDK5-p25:4.64 μM, CDK2-CyclinA:2.86 μM, CDK14-CyclinY:1.68 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.

Molecular Weight	505.08
Formula	C24H33ClN6O2S
CAS No.	2247481-21-4

Storage

keep away from direct sunlight,store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 16 mg/mL (31.68 mM), Sonification is recommended.

References and Literature

1. Beilei Wang, et al. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. Eur J Med Chem. 13 September 2018.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Cell Cycle Compound Library Kinase Inhibitor Library Hematonosis Compound Library Anti-Pancreatic Cancer Compound Library Covalent Inhibitor Library

Related Products

Related compounds with same targets

CDK4/6-IN-17 EHT 1610 Desmethylglycitein CDK8-IN-4 Tibremciclib Palbociclib Isethionate CDK4-IN-1 Ca2+ channel agonist 1

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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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.

Keywords

JSH-150 2247481-21-4 Cell Cycle/Checkpoint CDK inhibit Cyclin dependent kinase Inhibitor JSH 150 JSH150 inhibitor

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