| 货号 | 17130-5mg |
| 描述 | Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).1 Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol, allowing potent inhibition of HDACs 1, 2, 3, and 8 (IC50s = 53, 39, 53, and 26 nM, respectively), with less potency against HDACs 4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively).2,3 Through its effects on HDACs, romidepsin has anti-cancer activities, particularly against certain T cell lymphomas.4,5,6 |
| 别名 | FK228;FR901228;Istodax®;NSC 630176; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Nakajima, H.,Kim, Y.B.,Terano, H., et al. FR901228, a potent antitumor antibiotic, is a novel histone descetylase inhibitor. Experimental Cell Research 241, 126-133 (1998). 2.Wang, C.,Henkes, L.M.,Doughty, L.B., et al. Thailandepsins: Bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities. Journal of Natural Products 74(10), 2031-2038 (2011). 3.Mazitschek, R.,Patel, V.,Wirth, D.F., et al. Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorganic & Medicinal Chemistry Letters 18, 2809-2812 (2008). 4.Ueda, H.,Manda, T.,Matsumoto, S., et al. FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice. J.Antibiot.(Tokyo) 47(3), 315-323 (1994). 5.VanderMolen, K.M.,McCulloch, W.,Pearce, C.J., et al. Romidepsin (Istodaxr, NSC 630176, FR901228, FK228, depsipeptide): A natural product recently approved for cutaneous T-cell lymphoma. J.Antibiot.(Tokyo) 67(8), 525-231 (2015). 6.Coiffier, B.,Federico, M.,Caballero, D., et al. Therapeutic options in relapsed or refractory peripheral T-cell lymphoma. Cancer Treatment Reviews 40(9), 1080-1088 (2014). | |
| 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 | 540.7 |
| 分子式 | C24H36N4O6S2 |
| CAS号 | 128517-07-7 |
| 稳定性 | ≥ 2 years |
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