MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 ¦ÌM 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 ¦ÌM)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.

June 21, 2017

prudect name : MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 ¦ÌM 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 ¦ÌM)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.
MGCD0103 (Mocetinostat)

Synonyms: MGCD0103 (Mocetinostat)CAS NO: 726169-73-9Molecular Formula: C23H20N6OMolecular Weight: 396.44Purity: 98% minSolubility: In DMSOStorage: -20°C


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References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18533419