MS402

MS402 is an inhibitor of bromodomain 1 (BD1) of the bromodomain and extraterminal domain family of proteins (BET).¹ It selectively binds to BD1 over BD2 of bromodomain-containing protein 4 (BRD4; K_is = 77 and 718 nM, respectively) and, to a lesser extent, BD1 of BRD3 and BRD2 over BD2 of BRD3 and BRD2 (K_is = 110, 83, 200, and 240 nM, respectively). MS402 is also selective for BET BD1 over the additional bromodomain-containing proteins CREB-binding protein (CBP), p300/CBP-associated factor (PCAF), Brahma-related gene 1 (BRG1), also known as SMARCA4, nucleosome-remodeling factor subunit BPTF, and bromodomain adjacent to zinc finger domain protein 2B (BAZ2B; K_is = 775, 4,120, 6,560, 5,430, and 8,690 nM, respectively). It selectively inhibits the differentiation of isolated mouse CD4⁺ T cells into Th17 cells over Th1 cells, Th2 cells, or regulatory T cells (Tregs) when used at a concentration of 500 nM. MS402 (10 mg/kg twice per week) decreases disease severity and body weight loss in a mouse model of T cell transfer-induced colitis.

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1. Cheung, K., Lu, G., Sharma, R., et al. BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice. Proc. Natl. Acad. Sci. USA 114(11), 2952-2957 (2017).