| 应用 |
An HDAC inhibitor shown to inhibit angiogenesis and metastasis. |
| 产品介绍 |
Entinostat (MS-275)对HDAC1和HDAC3抑制作用强于与HDACs 4， 6， 8，和10，IC50分别为0.51 μM和1.7 μM。 |
| 备注 |
Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2. |
| 生化机理 |
MS-275 is an inhibitor of HDAC (histone deacetylase) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM). However, MS-275 does not inhibit HDAC8 (IC50 > 100 μM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin, inhibitors of poly (ADP-ribose) polymerase (PARP), or inhibitors of heat shock protein 90 (Hsp90). |
| 别名 |
SNDX-275;恩替诺特; N-[[4-[[(2-氨基苯基)氨基]甲酰]苯基]甲基]氨基甲酸 3-吡啶基甲基酯;MS-275; SNDX-275; MS 275; SNDX 275;A HDAC1 and HDAC3 inhibitor;3-pyridinylmethyl [[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]carbamate; N-(2-Aminophenyl)-4-[N-(pyridine-3ylmethoxycarbonyl)aminomethyl]benzamide |
