• Catalog Number:

  E1KS1122

• Amount:

  5mg1​ PHYSICAL AND CHEMICAL PROPERTIES

• Storage/Stability:

  at -20℃ 2 years

2​ Biological Activity MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively. In intact cells, MGCD0103 inhibited only a fraction of the total HDAC activity and showed long-lasting inhibitory activity even upon drug removal. MGCD0103 (Mocetinostat) induced hyperacetylation of histones, selectively induced apoptosis, and caused cell cycle blockade in various human cancer cell lines in a dose-dependent manner. MGCD0103 (Mocetinostat) 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 (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. [1] 3​ References: MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo Claire Bonfils, Yu Hou, et al. Mol Cancer Ther 2008;7:759-768 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.