Description | An inhibitor of BRD4 and class I and class IIb HDACs; inhibits BRD4 (IC50 = 0.71 µM), as well as class I HDACs (IC50s = 0.046, 0.058, 0.075, and 0.167 µM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 µM for HDAC6 and HDAC10, respectively); selective for these enzymes over BRD2, -3, and -T (IC50s = >20 µM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 µM for all); inhibits proliferation of HCT116, SW620, and DLD-1 cells (IC50s = 0.45, 1.78, and 2.11 µM, respectively); induces apoptosis and autophagy in HCT116 cells; reduces tumor growth in an HCT116 mouse xenograft model at 15 and 30 mg/kg |