| 货号 | 13284-1mg |
| 描述 | MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM).1 However, it does not inhibit HDAC8 (IC50 > 100 μM).1 MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo.23 Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin,4 inhibitors of poly (ADP-ribose) polymerase (PARP),5 or inhibitors of heat shock protein 90 (Hsp90).6 |
| 别名 | Entinostat;SNDX 275; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hu, E.,Dul, E.,Sung, C.M., et al. Identification of novel isoform-selective inhibitors within class I histone deacetylases. Journal of Pharmacology and Experimental Therapeutics 307, 720-728 (2003). 2.Saito, A.,Yamashita, T.,Mariko, Y., et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proceedings of the National Academy of Sciences of the United States of America 96, 4592-4597 (1999). 3.Jaboin, J.,Wild, J.,Hamidi, H., et al. MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors. Cancer Research 62, 6108-6115 (2002). 4.Xu, J.,Zhou, J.Y.,Wei, W.Z., et al. Sp1-mediated TRAIL induction in chemosensitization. Cancer Research 68(16), 6718-6726 (2008). 5.Gaymes, T.J.,Shall, S.,Macpherson, L.J., et al. Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica 94, 638-646 (2009). 6.Nguyen, A.,Su, L.,Campbell, B., et al. Synergism of heat shock protein 90 and histone deacetylase inhibitors in synovial sarcoma. Sarcoma (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 376.4 |
| 分子式 | C21H20N4O3 |
| CAS号 | 209783-80-2 |
| 稳定性 | ≥ 2 years |
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