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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $64 | In Stock | In Stock | |
| 10 mg | $98 | In Stock | In Stock | |
| 25 mg | $156 | In Stock | In Stock | |
| 50 mg | $239 | In Stock | In Stock | |
| 100 mg | $355 | In Stock | In Stock | |
| 200 mg | $526 | - | In Stock |
| 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]. |
| Synonyms | GTPL7512 |
| Molecular Weight | 414.91 |
| Formula | C20H19ClN4O2S |
| Cas No. | 916489-36-6 |
| Smiles | COC(=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 | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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