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Chemical Structure : MS417
CAS No.: 916489-36-6
Catalog No.: PC-62474Not For Human Use, Lab Use Only.
MS417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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MS417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.
MS417 shows 100-200-fold weaker affinity for CBP, BRD7, or BPTF, and no binding affinity for many other bromodomains.
MS417 blocks 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.
| M.Wt | 414.908 | |
| Formula | C20H19ClN4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Methyl 2-[(6S,Z)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetate |
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1. Zhang G, et al. J Biol Chem. 2012 Aug 17;287(34):28840-51.
2. Boehm D, et al. Cell Cycle. 2013 Feb 1;12(3):452-62.
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