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    Romidepsin，也稱為FK228或縮肽，是組蛋白脫乙酰酶(HDACs)的有效和選擇性抑制劑，HDACs與沉默的腫瘤抑制基因的再表達(dá)的調(diào)節(jié)有關(guān)。它是第一個(gè)表現(xiàn)出抗腫瘤活性的HDAC抑制劑，最初從日本土壤樣本中發(fā)現(xiàn)的桿狀革蘭氏陰性細(xì)菌紫色色桿菌中分離。Romidepsin對(duì)HDAC1和HDAC2酶(I類)表現(xiàn)出更強(qiáng)的抑制作用，與HDAC4和HDAC6酶(II類)相比，從N-末端組蛋白尾部的賴氨酸殘基中去除乙酰基，并保持更開放和轉(zhuǎn)錄活性的染色質(zhì)狀態(tài)。除了HDAC抑制作用，romidepsin還能夠在成人惡性腫瘤中誘導(dǎo)細(xì)胞周期停滯、細(xì)胞分化、凋亡和基因表達(dá)的改變。

產(chǎn)品性質(zhì)：

Cas No.：128517-07-7

別名：羅米地辛; FK 228; FR 901228; NSC 630176

化學(xué)名： (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone

Canonical SMILES CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

分子式：C24H36N4O6S2

分子量：540.7

溶解度：≥ 27.035mg/mL in DMSO, ≥ 35.27 mg/mL in EtOH with ultrasonic

儲(chǔ)存條件：Store at -20°C,unstable in solution, ready to use.

注意事項(xiàng)：

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References:

[1].Karen M VanderMolen, William McCulloch, Cedric J Pearce and Nicholas H Oberlies. Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma. The Journal of Antibiotics 2011: 64, 525-531

[2].Jyoti Panicker, Zhijie Li, Christine McMahon, Caroline Sizer, Kenneth Steadman, Richard Piekarz, Susan E. Bates and Carol J. Thiele. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. Cell Cycle 2010 9:9, 1830-1838