Romidepsin (FK228) peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

Romidepsin (FK228) is a naturally occurring bicyclic depsipeptide produced by Chromobacterium violaceum. This compound functions as a potent inhibitor of class I histone deacetylases (HDACs), enzymes involved in chromatin remodeling and gene expression regulation. FK228 undergoes intracellular activation via esterase-mediated hydrolysis, releasing a reactive aldehyde moiety that contributes to its biological activity.

At the molecular level, FK228 induces hyperacetylation of histones H3 and H4, leading to chromatin relaxation and modulation of gene transcription. The compound demonstrates time-dependent effects on histone acetylation, with peak activity observed within hours of treatment. Biochemical analyses reveal that FK228 treatment alters expression patterns of various proteins, including upregulation of pro-apoptotic Bax and downregulation of anti-apoptotic Bcl-2, ultimately promoting caspase-3-mediated apoptosis. The compound's stability and bioavailability allow for effective tissue penetration following oral administration.

• Furumai R, Matsuyama A, Kobashi N, Lee KH, Nishiyama M, Nakajima H, Tanaka A, Komatsu Y, Nishino N, Yoshida M, Horinouchi S. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21. PMID: 12208741.
• Lai MT, Yang CC, Lin TY, Tsai FJ, Chen WC. Depsipeptide (FK228) inhibits growth of human prostate cancer cells. Urol Oncol. 2008 Mar-Apr;26(2):182-9. doi: 10.1016/j.urolonc.2007.01.020. Epub 2007 Nov 19. PMID: 18312939.

Trifluoroacetic acid (TFA) is a common counterion from the purification process using High-Performance Liquid Chromatography (HPLC). The presence of TFA can affect the peptide's net weight, appearance, and solubility.

Impact on Net Weight: The TFA salt contributes to the total mass of the product. In most cases, the peptide content constitutes >80% of the total weight, with TFA accounting for the remainder.

Solubility: TFA salts generally enhance the solubility of peptides in aqueous solutions.

In Biological Assays: For most standard in vitro assays, the residual TFA levels do not cause interference. However, for highly sensitive cellular or biochemical studies, please be aware of its presence.