Romidepsin (FK228, depsipeptide)）| CAS#128517-07-7 APExBIO貨號A8173
乙醯化酶 (histone deacetylases ,HDAC)系列商品->>Romidepsin (FK228, depsipeptide)
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Romidepsin (FK228, depsipeptide)） | CAS#128517-07-7 APExBIO貨號A8173
HDAC1/HDAC2，強效和選擇性抑制劑
羅米地辛(Romidepsin)，也稱為 FK228 或縮肽(depsipeptide)，是組蛋白去乙醯化酶 (histone deacetylases ,HDAC) 的強效選擇性抑制劑，它與沈默的腫瘤抑制基因(tumor suppressor genes)的重新表達的調節有關。它是第一個表現出抗腫瘤活性(anti-tumor activity)的 HDAC 抑制劑(HDAC inhibitor)，最初是從日本土壤樣本中發現的一種桿狀革蘭氏陰性細菌紫色色桿菌(rod-shaped Gram-negative bacterium)中分離出來的。與 HDAC4 和 HDAC6 酶（II 類）相比，Romidepsin 對 HDAC1 和 HDAC2 酶（I 類）表現出更強的抑制作用，從 N 末端組蛋白尾(N-terminal histone tails)的賴氨酸殘基(lysine residues)中去除乙醯基，並保持更開放和轉錄活性更高的染色質(chromatin) 狀態。除了抑制 HDAC，romidepsin 還能夠在成人惡性腫瘤中誘導細胞週期停滯(cell cycle arrest)、細胞分化(cellular differentiation)、細胞凋亡(apoptosis)和基因表達(gene expression)的改變。
| 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 |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
- 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
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