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Romidepsin,HDAC1和HDAC2抑制剂

强大的HDAC1和HDAC2抑制剂
规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
R125265-1mg
 1mg 现货 Stock Image
R125265-5mg
 5mg 现货 Stock Image
R125265-25mg
 25mg 现货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
查看相关系列
histone deacetylase 1 Inhibitor histone deacetylase 2 Inhibitor histone deacetylase 3 Inhibitor histone deacetylase 4 Inhibitor histone deacetylase 5 Inhibitor histone deacetylase 6 Inhibitor histone deacetylase 7 Inhibitor histone deacetylase 8 Inhibitor histone deacetylase 9 Inhibitor
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基本描述

规格或纯度 ≥98%
英文名称 Romidepsin (FK228, Depsipeptide)
别名 罗咪酯肽|罗米地辛
英文别名 Romidepsin|Istodax|Depsipeptide|Chromadax|FK228|128517-07-7|Antibiotic FR 901228|FR901228|FK 228|FK-228|FR 901228|NSC-630176|FR-901228|romidepsina|romidepsine|romidepsinum|NSC 630176|CHEBI:61080|CX3T89XQBK|CHEMBL343448|(1S,4S,7Z,10S,16E,21R)-7-ethylidene-
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, althoμgh 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 promotes apoptosis in chronic lymphocytic leukemia (CLL) cells at a concentration corresponding to that at which H3 and H4 acetylation and HDAC inhibition occurs, selectively involving activation of caspase 8 and effector caspase 3, as well as down-regulation of c-FLIP protein.Potent HDAC1 and HDAC2 inhibitor (IC 50 values are 36 and 47 nM at HDAC1 and HDAC2 respectively). Induces apoptosis, cell-cycle arrest and modulates cytokine expression in cancer cells. Antitumor agent. Active in vivo and in vitro .
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，这些产品最多可以使用一周。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
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)。

Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.

名称和标识符

IUPAC Name (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
INCHI InChI=1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1
InChi Key OHRURASPPZQGQM-GCCNXGTGSA-N
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
RTECS YV9399000
PubChem CID 5352062
分子量 540.7

化学和物理性质

溶解性 DMSO 10 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

安全和危险性（GHS）

象形图
ghs06

Toxic

ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful
信号词 Danger
危险声明 H301: Toxic if swallowed
H341: Suspected of causing genetic defects
H317: May cause an allergic skin reaction
H400: Very toxic to aquatic life
H410: Very toxic to aquatic life with long lasting effects
预防措施声明 P261,P273,P280,P302+P352,P321,P405,P501,P264,P281,P270,P272,P333+P313,P362+P364,P391,P330,P203,P301+P316,P318
RTECS YV9399000

关联配体

Ligand ID 7006
名称 romidepsin
别名 FK228
类别 Synthetic organic
学名 (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-bis(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
生物活性评价 Romidepsin has the highest pKi value against HDAC1. Rank order of pKi is HDAC1>HDAC2>HDAC3=HDAC8>HDAC6>HDAC4>>HDAC5>>HDAC9>HDAC7 . HDAC1 has been tagged as the drug's primary target for data retrieval purposes only and in no way infers that this is the only target of this drug.
评价 Romidepsin is an anticancer agent originally isolated from the bacterium Chromobacterium violaceum, but subsequently produced synthetically. Romidepsin is an inhibitor of Class II histone deacetylases (HDACs).

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参考文献

1. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R.  (2010)  Chemical phylogenetics of histone deacetylases..  Nat Chem Biol,  6  (3):  (238-243).  [PMID:20139990]
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