HR488B is a potent, selective HDAC1 inhibitor with IC50 of 1.24 uM, effectively inhibits the proliferation of CRC cells.
HR488B exhibits a substantially stronger inhibitory effect against HCT116 (IC50 = 0.17 μM) and HT29 (IC50 = 0.59 μM) than SAHA (IC50 = 2.13 μM).
HR488B exhibits good selectivity against HDAC1 over HDAC2 (IC50 = 1.24 nM against HDAC1, IC50 = 10.42 nM against HDAC2), and shows low activity against HDAC8 (IC50 > 10 μM) and HDAC6 (IC50 > 10 μM).
HR488B (10 mg/kg/d) significantly suppresses the tumor growth in an HCT116 xenograft model.
