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MS417

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Catalog No. T16154Cas No. 916489-36-6
Alias GTPL7512

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

MS417

MS417

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Purity: 99.87%
Catalog No. T16154Alias GTPL7512Cas No. 916489-36-6
MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$64In StockIn Stock
10 mg$98In StockIn Stock
25 mg$156In StockIn Stock
50 mg$239In StockIn Stock
100 mg$355In StockIn Stock
200 mg$526-In Stock
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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:99.87%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.
Targets&IC50
CBP-BRD:32.7 μM, BRD4 BD2:46 nM , BRD4 BD1:30 nM
In vivo
BET (Bromodomain and Extra-Terminal domain)-specific bromodomain inhibitor MS417, designed to block BRD4 binding to the acetylated NF-κB, effectively attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα or infected by HIV.?MS417 ameliorates inflammation and kidney injury in HIV-1 transgenic mice, an animal model for HIVAN[1].
SynonymsGTPL7512
Chemical Properties
Molecular Weight414.91
FormulaC20H19ClN4O2S
Cas No.916489-36-6
SmilesCOC(=O)C[C@@H]1N=C(c2c(C)c(C)sc2-n2c(C)nnc12)c1ccc(Cl)cc1
Relative Density.1.43 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 50 mg/mL (120.51 mM), Sonication is recommended.
Solution Preparation Table
Ethanol
1mg5mg10mg50mg
1 mM2.4102 mL12.0508 mL24.1016 mL120.5081 mL
5 mM0.4820 mL2.4102 mL4.8203 mL24.1016 mL
10 mM0.2410 mL1.2051 mL2.4102 mL12.0508 mL
20 mM0.1205 mL0.6025 mL1.2051 mL6.0254 mL
50 mM0.0482 mL0.2410 mL0.4820 mL2.4102 mL
100 mM0.0241 mL0.1205 mL0.2410 mL1.2051 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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