Romidepsin
Romidepsin is a depsipeptide prodrug that inhibits histone deacetylases (HDACs). Romidepsin is currently in clinical trials as a potential treatment for T-cell lymphomas; it displays anticancer chemotherapeutic and antiviral activities. Romidepsin enhances in vitro and in vivo natural killer (NK) cell cytotoxicity by increasing MIC A/B (NK ligand) expression on tumor cells in leukemia and lymphoma models. Romidepsin also induces G0/G1 phase cell cycle arrest and apoptosis, upregulates expression of p21 and p53, downregulates expression of MMP2 and MMP9, and inhibits cell proliferation in non-small cell lung cancer (NSCLC) cells. In vitro, this product also induces HIV expression from infected CD4+ T cells, decreasing persistent latent HIV reservoirs.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18964425
| Cas No. |
128517-07-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H36N4O6S2 |
| Formula Wt. |
540.70 |
| IUPAC Name |
(1S,4S,7Z,10S,21R)-7-Ethylidene-4,21-diisopropyl-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone |
| Synonym |
FK228, Istodax, Depsipeptide, FR901228 |
| Appearance |
White to off white powder |
Foss F, Coiffier B, Horwitz S, et al. Tolerability to romidepsin in patients with relapsed/refractory T-cell lymphoma. Biomark Res. 2014 Sep 8;2:16. PMID: 25279222.
Satwani P, Bavishi S, Saha A, et al. Upregulation of NKG2D ligands in acute lymphoblastic leukemia and non-Hodgkin lymphoma cells by romidepsin and enhanced in vitro and in vivo natural killer cell cytotoxicity. Cytotherapy. 2014 May 20. [Epub ahead of print]. PMID: 24856896.
Wei DG, Chiang V, Fyne E, et al. Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing. PLoS Pathog. 2014 Apr 10;10(4):e1004071. PMID: 24722454.
Karthik S, Sankar R, Varunkumar K, et al. Romidepsin induces cell cycle arrest, apoptosis, histone hyperacetylation and reduces matrix metalloproteinases 2 and 9 expression in bortezomib sensitized non-small cell lung cancer cells. Biomed Pharmacother. 2014 Apr;68(3):327-34. PMID: 24485799.
Ueda H, Nakajima H, Hori Y, et al. FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. I. Taxonomy, fermentation, isolation, physico-chemical and biological properties, and antitumor activity. J Antibiot (Tokyo). 1994 Mar;47(3):301-10. PMID: 7513682.
