Catalog No. A8173

Romidepsin (FK228, depsipeptide)

(别名:Romidepsin; 罗米地辛

选择性的HDAC1/HDAC2抑制剂

Romidepsin (FK228, depsipeptide)
规格价格货期数量
1mL(10 mM in DMSO)
¥2636.00
现货
1mg
¥909.00
现货
5mg
¥2545.00
现货
CAS号:128517-07-7纯度:99.14%
仅用于科研,不用于诊疗。未经明确授权不得转售。
A
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特色产品

Annexin V-FITC/PI Apoptosis Kit
Annexin V-FITC/PI Apoptosis Kit
用于双染检测细胞凋亡和坏死
- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
Phos binding reagent (Phosbind) acrylamide
Phos binding reagent (Phosbind) acrylamide
分离和检测磷酸化/非磷酸化蛋白
- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
Cell Counting Kit-8 (CCK-8)
Cell Counting Kit-8 (CCK-8)
用于细胞增殖和细胞毒性试验
- 比MTT,MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单,无需有机溶剂
Cy5 TSA Fluorescence System Kit
Cy5 TSA Fluorescence System Kit
Cy5荧光标记的酪胺信号放大系统
- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)
EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)
用于观察mRNA运送,定位,翻译
- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
HotStart™ 2X Green qPCR Master Mix
HotStart™ 2X Green qPCR Master Mix
用于荧光定量目标DNA或cDNA
- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性,操作简单
HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus
HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus
高效的Cy5修饰RNA转录试剂盒
- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述

Romidepsin(FK228,depsipeptide)是一种有效的和选择性的HDACs抑制剂。HDACs可以调控沉默性肿瘤抑制基因的表达。HDACs可以从组蛋白N端的赖氨酸残基上去除乙酰基,使染色质维持一个更加开放的转录活性状态。Romidepsin是第一个体现抗肿瘤活性的HDAC抑制剂,最初是从日本土壤样品中的棒状革兰氏阴性菌Chromobacterium violaceum中分离出来的。Romidepsin对HDAC1和HDAC2(I类)的抑制活性比HDAC4和HDAC6(II类)更强。除了抑制HDACs,romidepsin还可以诱导细胞周期停滞、细胞分化、细胞凋亡和成人恶性肿瘤中基因表达的变化。

参考文献:
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

产品性质

物理外观A solid
CAS号128517-07-7
分子式C24H36N4O6S2
分子量540.7
小分子别名Romidepsin
化学名称(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
溶解度≥27.04 mg/mL in DMSO; insoluble in H2O; ≥35.27 mg/mL in EtOH with ultrasonic
SMILESCC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C
存储条件-20°C
运输条件蓝冰

产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)

IC50和靶点

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HDAC1HDAC2
生物活性数据36 nM47 nM

生物相关数据

质量控制

操作说明

APExBIO 顾客使用本产品发表的 14 篇科研文献

1. Hongyu Zhang, Baojin Zhou, et al. "Multidimensional Proteomics Reveals the Pro-apoptotic Mechanism of Platycodin D: Targeting RFC4 to Regulate the Notch Signaling Axis in Non-Small Cell Lung Cancer." Mol Cell Proteomics. 2026 May 15:101587. PMID: 42142580

2. Linmao Sun, Yufeng Liu, et al. "Acetylation-dependent regulation of core spliceosome modulates hepatocellular carcinoma cassette exons and sensitivity to PARP inhibitors." Nat Commun. 2024 Jun 18;15(1):5209. PMID: 38890388

3. Amy E Neely, Laura A Blumensaadt, et al. "NUP98 and RAE1 sustain progenitor function through HDAC-dependent chromatin targeting to escape from nucleolar localization." Commun Biol. 2023 Jun 23;6(1):664. PMID: 37353594

4. Rie Hagiwara, Kazunori Kageyama, et al. "Involvement of histone deacetylase 1/2 in adrenocorticotropic hormone synthesis and proliferation of corticotroph tumor AtT-20 cells." Peptides. 2020 Nov 9;136:170441. PMID: 33181265

5. Kulpa DA, Talla A, et al. "Differentiation to an effector memory phenotype potentiates HIV-l latency reversal in CD4+ T cells." J Virol. 2019 Oct 2. pii: JVI.00969-19. PMID: 31578289

6. Tang Y, Yu W. "SIRT1 and p300/CBP regulate the reversible acetylation of serine-threonine kinase NDR2." Biochem Biophys Res Commun. 2019 Aug 16. pii: S0006-291X(19)31586-4. PMID: 31427083

7. Tiffany C. Chang, Margarite D. Matossian, et al. "Evaluation of deacetylase inhibition in metaplastic breast carcinoma using multiple derivations of preclinical models of a new patient-derived tumor." bioRxiv. 2019 November 29

8. Kim SR, Lewis JM, et al. "BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or HDAC inhibition." Oncotarget.2018 Jun 26;9(49):29193-29207. PMID: 30018745

9. Nakano Y, Kelly MC, et al. "Defects in the Alternative Splicing-Dependent Regulation of REST Cause Deafness." Cell. 2018 Jul 26;174(3):536-548.e21. PMID: 29961578

10. Ho CF, Bon CP, et al. "Expression of DHA-Metabolizing Enzyme Alox15 is Regulated by Selective Histone Acetylation in Neuroblastoma Cells." Neurochem Res. 2017 Dec 12. PMID: 29235036

11. Tarasenko N, Chekroun-Setti H, et al. "COMPARISON OF THE ANTICANCER PROPERTIES OF A NOVEL VALPROIC ACID PRODRUG TO LEADING HISTONE DEACETYLASE INHIBITORS." J Cell Biochem. 2017 Nov 14. PMID: 29135083

12. Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID: 28110187

13. a RC, Popova EY, et al. "Histone Deacetylase 1 Is Essential for Rod Photoreceptor Differentiation by Regulating Acetylation at Histone H3 Lysine 9 and Histone H4 Lysine 12 in the Mouse Retina." J Biol Chem. 2017 Feb 10;292(6):2422-2440. PMID: 28028172

14. Li QQ, Hao JJ, et al. "Histone deacetylase inhibitor-induced cell death in bladder cancer is associated with chromatin modification and modifying protein expression: A proteomic approach." Int J Oncol. 2016 Jun;48(6):2591-607. PMID: 27082124

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