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Romidepsin,HDAC1和HDAC2抑制剂

Romidepsin (FK228, Depsipeptide) （订货以英文为准）

编号：R125265
CAS号：128517-07-7
分子式：C24H36N4O6S2
分子量：540.70
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R125265-1mg 阿拉丁 1mg ¥637.90
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R125265-5mg 阿拉丁 5mg ¥2276.90
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R125265-25mg 阿拉丁 25mg ¥6487.90
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产品名称 Romidepsin (FK228, Depsipeptide)
中文名称 Romidepsin,HDAC1和HDAC2抑制剂
CAS号 128517-07-7
MDL编码 MFCD18433404
分子式（M.F.） C24H36N4O6S2
分子量（M.W.） 540.70
储存条件 -20°C储存
溶解性DMSO 10 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件储存温度-20°C
应用选择性的HDAC1/HDAC2抑制剂
产品介绍Romidepsin (FK 228) 是具有抗肿瘤活性的组蛋白去乙酰化酶 (HDAC) 抑制剂，抑制 HDAC1，HDAC2，HDAC4 和 HDAC6，IC50 值分别为 36 nM，47 nM，510 nM 和 1.4 μM。Romidepsin (FK 228) 由紫色杆菌产生，诱导 G2/M 细胞周期阻滞和凋亡 (apoptosis)。
备注Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM, respectively.
生化机理Romidepsin, a selective inhibitor of histone deacetylases (HDACs), was approved for the treatment of cutaneous T-cell lymphoma in November 2009 by the U.S. FDA. Romidepsin is a member of a new class of antineoplastic agents active in T-cell lymphoma, the histone deacetylase inhibitors. Romidepsin strongly down-regulated expression of the immunosuppressive cytokine, interleukin (IL)-10, frequently overexpressed in CTCL, at both the RNA and protein level in CTCL cell lines and at the RNA level in primary CTCL cells. Romidepsin also increased expression of IFNG RNA and decreased expression of IL-2 and IL-4 RNA, although to a lesser extent compared to IL-10. Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively. Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. Romidepsin
别名罗咪酯肽; 罗米地辛;L-缬氨酸, N-((3S,4E)-3-羟基-7-巯基-1-氧代-4-庚基)-D-戊基-D-半胱氨酸-(2Z)-2-氨基-2-丁烯氧基-, (4-1)-内酯,环状(1-2)-二硫化物, 环[(2Z)-2-氨基-2-丁烯酰基-L-戊基-(3S,4E)-3-羟基-7-巯基-4-庚烯酰基-D-戊基-D-半胱氨酰]环状(35)-二硫化物; 缩酚酸肽;FK 228; FR 901228; NSC 630176; depsipeptide
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