MPT0E028

MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively[1]. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity[2].

HDAC1: 53.0 nM (IC₅₀); HDAC2: 106.2 nM (IC₅₀); HDAC6: 29.5 nM (IC₅₀); HDAC8: 2532.6 nM (IC₅₀)

[1] Huang HL, et al. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. DOI:10.1371/journal.pone.0043645
[2] Huang HL, et al. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6(7):4976-91. DOI:10.18632/oncotarget.3213