Mocetinostat
Cat. No.:YN270149
CAS No. :726169-73-9
产品名称: | Mocetinostat |
CAS No.: | 726169-73-9 |
Chemical Name: | N-(2-aminophenyl)-4-[[[4-(3-pyridinyl)-2-pyrimidinyl]amino]methyl]-benzamide |
Synonyms: | MGCD0103 |
分子量: | 396.44 |
分子式: | C₂₃H₂₀N₆O |
SMILES: | O=C(C1=CC=C(C=C1)CNC2=NC=CC(C3=CC=CN=C3)=N2)NC4=CC=CC=C4N |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Mocetinostat (MGCD0103)是一种有效,可口服和同种型选择性的HDAC (Class I/IV)抑制剂,抑制HDAC1,HDAC2,HDAC3和HDAC11的IC50分别为0.15,0.29,1.66 和 0.59 μM。 Mocetinostat对HDAC4,HDAC5,HDAC6,HDAC7或HDAC8没有抑制作用。 |
IC50和靶点: | [{name:"HDAC1:0.15 μM (IC50)"},{name: "HDAC2:0.29 μM (IC50)"},{name: "HDAC11:0.59 μM (IC50)"},{name: "HDAC3:1.66 μM (IC50)"}] |
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Fournel, M., Bonfils, C., Hou, Y., et al.MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivoMol. Cancer Ther.7(4),759-768(2008)
Marson, C.M., Matthews, C.J., Atkinson, S.J., et al.Potent and selective inhibitors of histone deacetylase-3 containing chiral oxazoline capping groups and a N-(2-aminophenyl)-benzamide binding unitJ. Med. Chem.58(17),6803-6818(2015)
Bonfils, C., Kalita, A., Dubay, M., et al.Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assayClin. Cancer Res.14(11),3441-3449(2008)
Nural-Guvener, H., Zakharova, L., Feehery, L., et al.Anti-fibrotic effects of class I HDAC inhibitor, mocetinostat is associated with IL-6/Stat3 signaling in ischemic heart failureInt. J. Mol. Sci.16(5),11482-11499(2015)