JSH-150

For research use only.

Catalog No.S8783

JSH-150 Chemical Structure

CAS No. 2247481-21-4

JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.

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Biological Activity

Description JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
Targets
CDK9 [1]
(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.[1]

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.[1]

Protocol

Kinase Assay:

[1]

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The ADP-Glo kinase assay:

The kinase reaction system contains 4.5 μL of CDK9/CyclinK kinase (3 ng/μL), 0.5 μL of serially diluted compounds 11-43 (including JSH-150), and 5 μL of CDK9 substrate PDKtide (0.2 μg/μL) with 10 μM ATP. The reaction in each tube is started immediately by adding ATP and keeps going for an hour under 37 °C. After the tube is cooled for 5 min at room temperature, 5 μL solvent reactions are carried out in a 384-well plate. Then 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ADP within 40 min. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 30 min to produce a luminescence signal. Luminescence signal is measured with an automated plate reader and the dose−response curve is fitted using Prism 7.0.
Cell Research:

[1]

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  • Cell lines: MV4-11, HL-60 and MEC-1 cells
  • Concentrations: serially diluted/various concentrations
  • Incubation Time: 2 h
  • Method:

    Signaling Pathway Study. MV4-11, HL-60 and MEC-1 cells are treated with DMSO, serially diluted JSH-150, 1 μM compound 7 for 2 h. Cells are then washed in 1 × PBS and lysed in cell lysis buffer. Phospho-CDK9 (Thr186), CDK9, Phospho-RNA Pol II (Ser2), Phospho-RNA Pol II (Ser5), RNA Pol II, XIAP, MCL-1, C-MYC, BCL-2 and GAPDH antibody are used for immunoblotting.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female nu/nu mice, Sprague-Dawley rats and beagle dogs
  • Dosages: 3 mg/kg, 10 mg/kg, 20 mg/kg, 2 mg/kg
  • Administration: IV, Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (197.98 mM)
Water 100 mg/mL (197.98 mM)
Ethanol '''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 505.08
Formula

C24H33ClN6O2S

CAS No. 2247481-21-4
Storage powder
in solvent
Synonyms N/A
Smiles COCCNC1CCC(CC1)NC2=NC=C(C(=C2)C3=CSC(=N3)NCC4(CCOCC4)C#N)Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID