MS402 是一种 BD1 选择性的 BET BrD 抑制剂，对 BRD4(BD1)，BRD4(BD2)，BRD3(BD1)， BRD3(BD2)， BRD2(BD1) 和 BRD2(BD2) 的 Ki 分别为 77 nM，718 nM，110 nM，200 nM，83 nM 和 240 nM。MS402 阻断 Th17 细胞分化并改善小鼠结肠炎。
货号:ajcx38714
CAS:1672684-68-2
分子式:C20H19ClN2O3
分子量：370.83
溶解度:DMSO : 100 mg/mL (269.67 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice[1].

Reconstitution with naÏve 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[1].

[1]. Cheung K, et al. BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957.

Protocol:

BRD4-BD1 77nM(Ki)

BRD2-BD1 83nM(Ki)

BRD3-BD1 110nM(Ki)

BRD3-BD2 200nM(Ki)

BRD2-BD2 240nM(Ki)

BRD4-BD2 718nM(Ki)