Imofinostat

Imofinostat is an inhibitor of histone deacetylase 1 (HDAC1), -2, and -6 (IC₅₀s = 53, 106.2, and 29.5 nM, respectively).¹ It is selective for HDAC1, -2, and -6 over HDAC8 and -4 (IC₅₀s = 2,532 and >10,000 nM, respectively). Imofinostat increases the acetylation and activity of MAPK 1 in WI38 human lung fibroblasts at 1 µM and reduces connective tissue growth factor (CTGF), α-smooth muscle actin (α-SMA), and fibronectin in the same cells when stimulated by TGF-β.² It decreases lung fibrosis in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877) at 25-100 mg/kg. It induces cell cycle arrest at the G₀/G₁ phase and apoptosis in HCT116 colorectal cancer and Ramos (RA 1) B cell lymphoma cells.^1,3 Imofinostat (50-200 mg/kg) reduces tumor growth in HCT116 and BJAB B-cell lymphoma mouse xenograft models and increases survival in a Ramos (RA 1) mouse xenograft model.

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1. Huang, H.-L., Lee, H.-Y., Tsai, A.-C., 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 7(8), e43645 (2012).

2. Liu, C.H., Lee, H.S., Liou, J.P., et al. MPT0E028, a novel pan-HDAC inhibitor, prevents pulmonary fibrosis through inhibition of TGF-β-induced CTGF expression in human lung fibroblasts: Involvement of MKP-1 activation. Eur. J. Pharmacol. 977, 176711 (2024).

3. Huang, H.L., Peng, C.Y., Lai, M.J., et al. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget 6(7), 4976-4991 (2015).