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Mocetinostat (MGCD0103)

Catalog No. S1122 5 5 6 Customer Review(s) Product Citations9 Product Citation(s)
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Mocetinostat (MGCD0103) Chemical Structure

Bio Information

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] 

 

References:

[1] Mol Cancer Ther 2008;7:759-768

Chemical Information

Molecular Weight (WM): 396.44
Formula:

C23H20N6O

Solubility(R.T.:25°C): DMSO 13mg/mL 
Water <1mg/mL 
Ethanol <1mg/mL 

Quality Control

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H-NMR HPLC

Research Area

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Mocetinostat (MGCD0103) has been referenced in 9 publications.

Acetylation limits 53BP1 association with damaged chromatin to promote homologous recombination.
Selective class I histone deacetylase inhibition suppresses hypoxia-induced cardiopulmonary remodeling through an antiproliferative mechanism.
The HDAC class I-specific inhibitor entinostat (MS-275) effectively relieves epigenetic silencing of the LAT2 gene mediated by AML1/ETO.
C-terminal binding protein-2 regulates response of epithelial ovarian cancer cells to histone deacetylase inhibitors.
An “exacerbate-reverse” strategy in yeast identifies Histone deacetylase inhibition as a correction for cholesterol and sphingolipid transport defects in human Niemann-Pick type C disease.
Evidence for a link between histone deacetylation and Ca2 {+} homoeostasis in sphingosine-1-phosphate lyase-deficient fibroblasts.
Inhibition of Multiple Pathogenic Pathways by Histone Deacetylase Inhibitor SAHA in a Corneal Alkali-Burn Injury Model.
Inhibition of Histone deacetylases 1 and 6 enhances cytarabine-induced apoptosis in pediatric acute myeloid leukemia cells.
Class I and Class II Histone Deacetylases Are Potential Therapeutic Targets for Treating Pancreatic Cancer.

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Average Customer Review

(6 customer reviews)
  • ;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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