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Nanatinostat is an inhibitor of histone deacetylases (HDACs).1 It selectively inhibits HDAC1, HDAC2, and HDAC3 over HDAC5 and HDAC6 (IC50s = 3, 4, 7, 200, and 2,100 nM, respectively). Nanatinostat inhibits proliferation in a panel of 15 cancer cell lines (GI50s = 31-750 nM). It induces cell cycle arrest at the sub-G1 and G2/M phases and induces apoptosis in HCT116 colorectal cancer cells when used at a concentration of 3 µM. Nanatinostat (50 mg/kg per day) decreases tumor volume in an HCT116 mouse xenograft model.
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1. Discovery of 2-