Mocetinostat

Mocetinostat (CAS 726169-73-9) inhibits class 1 isoforms of HDAC, specifically HDAC1 (IC50=0.15 µM), HDAC2 (IC50=0.29 µM) and HDAC3 (IC50=1.66 µM), which may result in epigenetic changes in tumor cells and so tumor cell death. It exhibited potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines (IC50 from 0.09-20 µM) in vitro, and HDAC inhibitory activity was required for these effects. In vivo, Mocetinostat significantly inhibited growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors.

MGCD0103

Synonyms: MGCD-0103; Mocetinostat
Technical Data: Molecular Weight - 396.46; Molecular formula - C23H20N6O; CAS No - 726169-73-9

Ordering Information: Product Number - EC-000.2284
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References:
1. Chia K, et al. The histone deacetylase inhibitor MGCD0103 has both deacetylase and microtubule inhibitory activity. Mol Pharmacol. 2010 Jun 10.
2. Prince HM, et al. Clinical studies of histone deacetylase inhibitors. Clin Cancer Res. 2009 Jun 15;15(12):3958-69.
3. Marielle Fournel, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther 2008;7(4).

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Related service: collection of Histone Deacetylase Inhibitors.