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Droxinostat is an inhibitor of histone deacetylase (HDAC) 3, 6, and 8 (IC50s = 16.9, 2.47, and 1.46 μM, respectively).1 It is selective for HDAC3, 6, and 8 over HDAC1, 2, 7, 9, and 10 (IC50s = >20 μM). Droxinostat increases histone H3 and H4 acetylation in PPC-1 prostate, OVCAR3 ovarian, U937 leukemia, HT-29 colon, and T47D breast cancer cells. It also inhibits proliferation and colony formation of SMMC-7721 and HepG2 hepatocellular carcinoma cell lines via activation of mitochondrial apoptosis and reduction of cellular FLICE-inhibitory protein (c-FLIP).2
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1. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol. Cancer Ther. 9(1), 246-256 (2010).
2. Droxinostat, a histone deacetylase inhibitor, induces apoptosis in hepatocellular carcinoma cell lines via activation of the mitochondrial pathway and downregulation of FLIP. Transl. Oncol. 9(1), 70-78 (2016).