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JSH-150

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Catalog No. T8484Cas No. 2247481-21-4

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

JSH-150

JSH-150

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Purity: 99.96%
Catalog No. T8484Cas No. 2247481-21-4
JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$89In StockIn Stock
10 mg$156In StockIn Stock
25 mg$347In StockIn Stock
50 mg$538In StockIn Stock
100 mg$651-In Stock
500 mg$1,390InquiryInquiry
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Purity:99.96%
Appearance:Solid
Color:White to Red
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Product Introduction

Bioactivity
Description
JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
Targets&IC50
CDK7-CyclinH-MNAT1:1.72 μM, CDK9-CyclinT1:1 nM, CDK14-CyclinY:1.68 μM, CDK16-CyclinY:292 nM, CDK1-CyclinB:1.34 μM, CDK5-p25:4.64 μM, CDK2-CyclinA:2.86 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.
Chemical Properties
Molecular Weight505.08
FormulaC24H33ClN6O2S
Cas No.2247481-21-4
SmilesCOCCN[C@H]1CC[C@@H](CC1)Nc1cc(-c2csc(NCC3(CCOCC3)C#N)n2)c(Cl)cn1
Relative Density.1.29 g/cm3 (Predicted)
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 | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (494.97 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.96 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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

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