Mocetinostat

Mocetinostat is an orally available inhibitor of histone deacetylases (HDACs) that selectively targets HDAC1 and 2 (IC₅₀s = 0.15 and 0.29 µM, respectively), less potently inhibits HDAC3 and 11 (IC₅₀s = 1.66 and 0.59 µM, respectively) and has negligible actions against HDAC4-8.^1,2 It induces hyperacetylation of histones, causes cell cycle blockade, and induces apoptosis in cancer cells in vitro.^1,3 Mocetinostat also has antitumor activity in vivo, blocking the growth of human tumor xenografts in mice.¹ It also significantly reduces cardiac fibrosis following ischemic heart failure in mice.⁴

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1. Fournel, M., Bonfils, C., Hou, Y., et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol. Cancer Ther. 7(4), 759-768 (2008).

2. Marson, C.M., Matthews, C.J., Atkinson, S.J., et al. Potent and selective inhibitors of histone deacetylase-3 containing chiral oxazoline capping groups and a N-(2-aminophenyl)-benzamide binding unit. J. Med. Chem. 58(17), 6803-6818 (2015).

3. Bonfils, C., Kalita, A., Dubay, M., et al. Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay. Clin. Cancer Res. 14(11), 3441-3449 (2008).

4. Nural-Guvener, H., Zakharova, L., Feehery, L., et al. Anti-fibrotic effects of class I HDAC inhibitor, mocetinostat is associated with IL-6/Stat3 signaling in ischemic heart failure. Int. J. Mol. Sci. 16(5), 11482-11499 (2015).