Mocetinostat (726169-73-9) 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 Mocetinostat displays antifibrotic effects in ischemic heart failure.3 Attenuates the development of hypersensitivity in models of neuropathic pain.4 Active in vivo.5 类HDAC抑制剂mocetinostat(726169-73-9)是一类亚型选择性HDAC抑制剂,对HDAC1、2,3和11的ic50分别为0.15、0.29、1.66和0.59 μM 1 .诱导组蛋白高乙酰化,诱导肿瘤抑制因子p21WAF1表达,抑制人癌细胞增殖 摩替替他在缺血性心力衰竭中具有抗纤维化作用 减弱神经性疼痛模型中超敏反应的发展 活跃的体内。
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
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 from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT
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