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.