JSH-150
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MedKoo CAT#: 573173

CAS#: 2247481-21-4

Description: JSH-150 is a potent CDK9 inhibitor. JSH-150 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). JSH-150displayed 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.


Chemical Structure

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JSH-150
CAS# 2247481-21-4

Theoretical Analysis

MedKoo Cat#: 573173
Name: JSH-150
CAS#: 2247481-21-4
Chemical Formula: C24H33ClN6O2S
Exact Mass: 504.2074
Molecular Weight: 505.08
Elemental Analysis: C, 57.07; H, 6.59; Cl, 7.02; N, 16.64; O, 6.34; S, 6.35

Price and Availability

Size Price Availability Quantity
25.0mg USD 350.0 2 Weeks
50.0mg USD 650.0 2 Weeks
100.0mg USD 1050.0 2 Weeks
200.0mg USD 1650.0 2 Weeks
500.0mg USD 2450.0 2 Weeks
1.0g USD 3450.0 2 Weeks
2.0g USD 5450.0 2 Weeks
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Synonym: JSH-150; JSH 150; JSH150;

IUPAC/Chemical Name: 4-(((4-(5-chloro-2-((4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile

InChi Key: XSDZPPRQLIZLDG-WEBLMRDCSA-N

InChi Code: InChI=1S/C24H33ClN6O2S/c1-32-11-8-27-17-2-4-18(5-3-17)30-22-12-19(20(25)13-28-22)21-14-34-23(31-21)29-16-24(15-26)6-9-33-10-7-24/h12-14,17-18,27H,2-11,16H2,1H3,(H,28,30)(H,29,31)/t17?,18-

SMILES Code: COCCNC1CC[C@H](NC2=NC=C(Cl)C(C3=CSC(NCC4(C#N)CCOCC4)=N3)=C2)CC1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 505.08 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q. 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. 2018 Oct 5;158:896-916. doi: 10.1016/j.ejmech.2018.09.025. Epub 2018 Sep 13. PubMed PMID: 30253346.

JSH-150

25.0mg / USD 350.0


Additional Information

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 JSH-150 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.