Description
A BET family protein inhibitor; binds to BD1 in BRD2, BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively); binds to bromodomains of CBP and p300 (Kds = ~100 nM for both); inhibits CpG-induced proliferation of primary CLL cells from 0.1-10 µM; inhibits Ba/F3 cell-induced splenomegaly in mice from 0.5-10 mg/kg; reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models