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Romidepsin (FK228, depsipeptide)

现货
Catalog No.
A8173
选择性的HDAC1/HDAC2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,900.00
现货
1mg
¥ 1,100.00
现货
5mg
¥ 3,300.00
现货

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Background

Romidepsin, also known as FK228 or depsipeptide, is potent and selective inhibitor of histone deacetylases (HDACs) which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.

Reference

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

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

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt540.7
Cas No.128517-07-7
FormulaC24H36N4O6S2
SynonymsIstodax, Antibiotic FR 901228, FK228, FR 901228, FK-228,Romidepsin
Solubility≥27.035mg/mL in DMSO, ≥35.27 mg/mL in EtOH with ultrasonic, <2.99 mg/mL in H2O
Chemical 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
SDFDownload SDF
Canonical SMILESCC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验:

细胞系

人NB细胞(SMS-KCNR、SK-N-BE2、SH-SY5Y、SK-N-AS、L A1-15N、SH-SHEP 和IMR32细胞系)

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

72 h;IC50范围介于1-6.5 ng/ml之间。

应用

在MTT或MTS试验中,romidepsin(0.5-30 ng/mL)剂量依赖地减少所有NB细胞系的细胞活力。在不同NB细胞系中,romidepsin的IC50值介于1-6.5 ng/ml之间。通过光学显微镜的形态学检查表明,所有romidepsin处理的NB细胞系中,细胞数量剂量依赖性地减少,细胞形态向圆形、致密和非粘附细胞变化。

动物实验:

动物模型

正常裸鼠

剂量

1.0-10 kg/mL;i.v.;尾静脉注射

应用

在第0天时,Clolon 38和Colon 26通过皮下植入,M5076和Meth A通过腹腔植入小鼠体内,在第1天时给药,romidepsin显著抑制Clolon 38和M5076的生长,而对Colon26或Meth A不起作用。此外,当第4天、或第7或8天才开始给药时,romidepsin有效抑制Colon 38、M5076和Meth A的生长,其对M5076 和Meth A的作用比在第1天给药时更加有效。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Panicker J, Li Z, McMahon C, et al. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells[J]. Cell Cycle, 2010, 9(9): 1830-1838.

[2] Ueda H1, Manda T, Matsumoto S, Mukumoto S, Nishigaki F, Kawamura I, Shimomura K. FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice. J Antibiot (Tokyo). 1994 Mar;47(3):315-23.

生物活性

描述 Romidepsin (FK228,depsipeptide)是一种有效的和选择性的I类HDACs抑制剂,在无细胞试验中作用于HDAC1、HDAC2、HDAC4和HDAC6,IC50值分别为36、47、510和14000 nM。
靶点 HDAC1 HDAC2        
IC50 36 nM 47 nM        

质量控制

化学结构

Romidepsin

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