MS-402

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MS-402 (MS402) 是 BET 第一个溴结构域 (BRD4-BD1) 的有效、选择性抑制剂，Ki 为 77 nM。

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.

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Reconstitution with na?ve CD4+CD45RBhi cells isolated from spleen and lymph nodes of C57BL/6 mice, Rag1-/- mice begin losing weight after 4 week. MS402 (10 mg/kg; intraperitoneally twice a week for 3 weeks) shows much less weight loss. Animal Model:C57BL/6 mice, Rag1-/- mice with T-cell transfer-induced colitis model Dosage:10 mg/kg Administration:Intraperitoneally twice a week for 3 weeks Result:Showed much less weight loss.

MS402 | MS 402

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1672684-68-2

370.833

C20H19ClN2O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (269.67 mM)

O=C(NC1=CC=C(OC)C=C1)C2=CC=C(NC3=C(C)C(CC3)=O)C(Cl)=C2

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

(-20℃)

With Ice Pack

≥ 2 years