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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥2636.00 | 现货 | |
1mg | ¥909.00 | 现货 | |
5mg | ¥2545.00 | 现货 |
特色产品
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- 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
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- 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
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 |
SMILES | CC=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 |
SDF文件 | Download SDF |
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 | HDAC1 | HDAC2 |
生物活性数据 | 36 nM | 47 nM |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. 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
- 2. 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
- 3. 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.
- 4. 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
- 5. 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
- 6. 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
- 7. 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
- 8. 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
- 9. 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
- 10. 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
- 11. 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
- 12. 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