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MS-275 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC3 (IC50s = 0.3 and 8 µM, respectively).1 It is selective for HDAC1 and HDAC3 over HDAC8 (IC50 = >100 µM). MS-275 decreases the proliferation of A2780 ovarian, Calu-3 lung, HL-60 promyeloblast leukemia, and K562 chronic myeloid leukemia (CML) cells (IC50s = 0.0415, 0.195, 0.212, and 0.589 µM, respectively). It induces cell cycle arrest at the G1 phase in A2780 cells when used at a concentration of 1 µM. MS-275 (49 mg/kg per day) decreases tumor volume and increases intratumoral histone H4 acetylation in an HT-29 colon cancer mouse xenograft model.
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1. Identification of novel isoform-