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Chemical Structure : MS-402
Catalog No.: PC-70284Not For Human Use, Lab Use Only.
MS-402 (MS402) is a potent, selective inhibitor of the first bromodomain of BET (BRD4-BD1) with Ki of 77 nM.
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MS-402 (MS402) is a potent, selective inhibitor of the first bromodomain of BET (BRD4-BD1) with Ki of 77 nM; shows about 10-fold weaker affinity for BRD4-BD2 (Ki=718 nM) and CBP, and >50-fold for PCAF, SMARCA4, BPTF and BAZ2B; selectively blocks Th17 cell differentiation with a little or almost no effect on Th1 or Th2 and Treg cells; preferentially renders Brd4 binding to Th17 signature gene loci over those of housekeeping genes and reduces Brd4 recruitment of p-TEFb to phosphorylate and activate RNA polymerase II for transcription elongation; prevents and ameliorates T-cell transfer-induced colitis in mice.
| M.Wt | 370.833 | |
| Formula | C20H19ClN2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Cheung K, et al. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957.
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