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MS402

Chemical Structure : MS402

CAS No.: 1672684-68-2

MS402 (MS-402)

货号: PC-70284Not For Human Use, Lab Use Only.

MS402 (MS 402) is a potent, selective inhibitor of the first bromodomain of BET (BRD4-BD1) with Ki of 77 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MS402 (MS 402) is a potent, selective inhibitor of the first bromodomain of BET (BRD4-BD1) with Ki of 77 nM.
MS402 shows about 10-fold weaker affinity for BRD4-BD2 (Ki=718 nM) and CBP, and >50-fold for PCAF, SMARCA4, BPTF and BAZ2B.
MS402 selectively blocks Th17 cell differentiation with a little or almost no effect on Th1 or Th2 and Treg cells.
MS402 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.
MS402 prevents and ameliorates T-cell transfer-induced colitis in mice.

物理化学性质&存储条件

分子量 370.833
分子式 C20H19ClN2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-chloro-N-(4-methoxyphenyl)-4-((2-methyl-3-oxocyclopent-1-en-1-yl)amino)benzamide

参考文献

1. Cheung K, et al. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957.

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