Romidepsin (FK228, depsipeptide)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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
- 1. 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
- 2. 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.
- 3. 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
- 4. 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
- 5. 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
- 6. 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
- 7. 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
- 8. 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
- 9. 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
- 10. 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
- 11. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 540.7 |
| Cas No. | 128517-07-7 |
| Formula | C24H36N4O6S2 |
| Synonyms | Istodax, Antibiotic FR 901228, FK228, FR 901228, FK-228,Romidepsin |
| Solubility | ≥27.04 mg/mL in DMSO; insoluble in H2O; ≥35.27 mg/mL in EtOH with ultrasonic |
| 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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. |
|
| 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 | ||||
质量控制和MSDS
- 批次：
化学结构
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
相关生物数据
