Mocetinostat (MGCD-0103)

MGCD0103 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, MGCD0103 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.

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; Price and Availability: Inquire This product is also available to buy in bulk quantities.

Related Products: Suberoylanilide Hydroxamic Acid; MS-275 (Entinostat); CI-994 (Tacedinaline); BML-210; M344; PXD101 (Belinostat); LBH-589 (Panobinostat); Tubastatin A; Scriptaid; NSC 3852; NCH 51; HNHA; BML-281; CBHA; Salermide; Pimelic Diphenylamide; ITF2357 (Givinostat); PCI-24781; APHA Compound 8; Droxinostat; SB939.

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).