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Mocetinostat | Class I HDAC inhibitor

Mocetinostat (726169-73-6) is a class I, isoform-selective HDAC inhibitor, IC50s=0.15, 0.29, 1.66 and 0.59 μM for HDAC1, 2, 3 and 11 respectively.1 Induces hyperacetylation of histones, induces expression of the tumor suppressor p21WAF1 and inhibits proliferation of human cancer cells.2 Displays antifibrotic effects in ischemic heart failure.3 Attenuates the development of hypersensitivity in models of neuropathic pain.4 Active in vivo.5

References/Citations

1) Zhou et al. (2008), Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ulpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor; J. Med. Chem., 51 4072
2) Raeppel et al. (2009), SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4((4-(pyridine-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103); Bioorg. Med. Chem. Lett., 19 644
3) Nural-Guvener et al. (2015), Anti-Fibrotic Effects of Class I HDAC Inhibitor, Mocetinostat is Associated with IL-6/Stat3 Signaling in Ischemic Heart Failure; Int. J. Mol. Sci., 16 11482
4) Denk et al. (2013), HDAC inhibitors attenuate the development of hypersensitivity in models of neuropathic pain; Pain, 154 1668
5) Bonfils et al. (2008), Evaluation of the pharmacodynamics effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay; Clin. Cancer Res., 14 3441

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Focus Biomolecules cell signaling supplier, chemical structure of Mocetinostat | Class I HDAC inhibitor | CAS 726169-73-9

Catalog#  10-3306-0005

$70.00
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CAS:
726169-73-9
Catalog Number:
10-3306
Activity:
Class I HDAC inhibitor
Chemical Name:
N-(2-Aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide
Alternate Names:
MGCD0103
Molecular Weight:
396.44
Molecular Formula:
C23H20N6O
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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