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Mocetinostat
- MGCD 0103 - MG 0103
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H20N6O
- MW: 396.44
Description
Mocetinostat (MGCD 0103) is a class I-selective histone deacetylase inhibitor with activity against HDAC1, HDAC2, HDAC3 and HDAC11. It produces transcriptional and antiproliferative effects in hematologic and solid tumor models.
Class I HDACs regulate chromatin accessibility, cell-cycle control, differentiation and survival. Mocetinostat is useful for studying HDAC-dependent oncogenic transcription, epigenetic reprogramming and combination strategies in cancer pharmacology.
Key Features
- Class I-selective HDAC inhibitor
- Sub-micromolar activity reported at HDAC1, HDAC2 and HDAC11
- Weaker activity at class II HDACs in reported assays
- Broad antitumor activity reported in vitro and in vivo
Applications
- HDAC enzyme pharmacology
- Epigenetic cancer research
- Transcriptional regulation and differentiation studies
- Combination therapy and antiproliferative assays
More Information
| Parent CAS No. | 726169-73-9 |
|---|---|
| Chemical Name | N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide |
| SMILES | C(NC1=CC=CC=C1N)(=O)C1=CC=C(CNC2=NC=CC(C3=CC=CN=C3)=N2)C=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29) |
| InChiKey | HRNLUBSXIHFDHP-UHFFFAOYSA-N |
| CID | 9865515 |
| Short Description | HDAC inhibitor |
References
- T. Beckers et al. Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. Int J Cancer. 2007 Sep 1;121(5):1138-48.
- M. 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 Apr;7(4):759-68.
- N. Zhou et al. Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor. J Med Chem. 2008 Jul 24;51(14):4072-5.
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