| 应用 |
A potent inhibitor of HDAC1, HDAC2, HDAC3, and HDAC11. |
| 产品介绍 |
Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂，对HDAC1抑制作用最强，IC50为0.15 μM，比作用于HDAC2， 3，和11选择性高2到10倍，对HDAC4， 5， 6， 7，和8没有抑制活性。Phase 2。 |
| 备注 |
Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 1/2. |
| 生化机理 |
MGCD0103 potently inhibits a subset of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells. |
| 别名 |
N-(2-氨基苯基)-4-([[4-(吡啶-3-基)嘧啶-2-基]氨基]甲基)苯甲酰胺;MGCD0103;MGCD 0103;MGCD-0103;N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide |
