MS402

A BD1-selective BET inhibitor, selectively binds to BD1 over BD2 of BRD4 (Kis = 77 and 718 nM, respectively) and, to a lesser extent, BD1 of BRD3 and BRD2 over BD2 of BRD3 and BRD2 (Kis = 110, 83, 200, and 240 nM, respectively), selective for BET BD1 over CBP, PCAF, BRG1, BPTF, and BAZ2B (Kis = 775, 4,120, 6,560, 5,430, and 8,690 nM, respectively), selectively inhibits the differentiation of isolated mouse CD4+ T cells into Th17 cells over Th1 cells, Th2 cells, or Tregs at 500 nM, decreases disease severity and body weight loss in a mouse model of T cell transfer-induced colitis at 10 mg/kg twice per week