Mocetinostat

Aliases: Mocetinostat; N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide; MGCD010
Catalog No: 14136 Format: 25 mg $300 Buy
Catalog No: 14137 Format: 5 mg $80 Buy
Application: Histone Acetylation (HAT & HDAC)

Chemical Properties

MW = 396.4
C23H20N6O
CAS 726169-73-9
>98% (HPLC); NMR (Conforms)

Description

Class I, isoform-selective HDAC inhibitor (IC50 = 0.15, 0.29, 1.66 and 0.59 µM for HDAC1, 2, 3 and 11 respectively) (ref 1). Induces hyperacetylation of histones, induces expression of the tumor supressor p21WAF1 and inhibits proliferation of human cancer cells (ref 2). Displays antifibrotic effects in ischemic heart failure (ref 3). Attenuates the development of hypersensitivity in models of neuropathic pain (ref 4). Active in vivo (ref 5).

Contents

Off-white crystalline powder. May be dissolved in DMSO (25 mg/ml).

References

1. N Zhou et al. J. Med. Chem. 2008, 51:4072
2. S Raeppel et al. Bioorg. Med. Chem. Lett. 2009, 19:644
3. H Nural-Govener et al. Int. J. Mol. Sci. 2015, 16:11482
4. F Denk et al. Pain 2013, 154:1668
5. C Bonfils et al. Clin. Cancer Res. 2008, 14:3441

 
Chemical structure of Mocetinostat.

Chemical structure of Mocetinostat.