United States (Change Country)Mocetinostat (MGCD0103) Chemical Structure
Mocetinostat (MGCD0103) 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. Mocetinostat (MGCD0103) induced hyperacetylation of histones, selectively induced apoptosis, and caused cell cycle blockade in various human cancer cell lines in a dose-dependent manner. Mocetinostat (MGCD0103) 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 (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. [1]
[1] Mol Cancer Ther 2008;7:759-768
| Molecular Weight (WM): | 396.44 |
|---|---|
| Formula: | C23H20N6O |
| Solubility(R.T.:25°C): | DMSO 13mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL |
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;PLoS ONE 7(12), e52095 Mocetinostat (MGCD0103) purchased from Selleck
;Oncogene (2012), 1–8 Mocetinostat (MGCD0103) purchased from Selleck
Data from [PLoS ONE 2011;6, e17138] Mocetinostat (MGCD0103) purchased from Selleck
;Dr. Zhang of Tianjin Medical University Mocetinostat (MGCD0103) purchased from Selleck
Data from [PLoS ONE 2011;6, e17138] Mocetinostat (MGCD0103) purchased from Selleck
Data from [J Biol Chem 2011;286, 23842–23851] Mocetinostat (MGCD0103) purchased from Selleck
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