Description: |
MPT0E028 is a potent HDAC inhibitor that inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA; inhibits class I HDAC1, HDAC2, and class Iib HDAC6 with IC50 of 53, 106, and 29.5 nM, respectively, weakly inhibits HDAC8 (IC50=2.5 uM), but not for HDAC4 (IC50>10 uM); inhibits the growth of HCT116 and MDA-MB-231 cells with IC50 of 0.09 and 0.19 uM; inhibits HCT116 tumor xenograft in vivo without significant adverse effects, shows stronger anti-cancer efficacy than SAHA. |