Name: Romidepsin (FK228, depsipeptide)
Price: 528.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
- Properties
  - Alternative Name
    
    Istodax, Antibiotic FR 901228, FK228, FR 901228, FK-228, Romidepsin; (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
    
    CAS Number
    
    128517-07-7
    
    Molecular Formula
    
    C24H36N4O6S2
    
    Molecular Weight
    
    540.7
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥27.04 mg/mL in DMSO; insoluble in H2O; ≥35.27 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
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    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