brd4in2

BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC50 value of 9.9 nM.

PARP1/BRD4-IN-2 is a potent and selective inhibitor of PARP1 (IC50: 197 nM) and BRD4 (IC50: 238 nM), which inhibits DNA damage repair, blocks the G0/G1 cell cycle transition, and induces apoptosis. PARP1/BRD4-IN-2 exhibits antitumor effects in the MDA-MB-468 mouse xenograft tumor model and is used to study triple-negative breast cancer (TNBC).

PLK1/BRD4-IN-2 (compound 15), an analog of BI-2536, simultaneously inhibits both Polo-like kinase 1 (PLK1 IC 50 = 40 nM) and BRD4 bromodomain (BRD4-BD1 IC 50 = 28 nM) as a dual inhibitor [1].