Decanoyl-RVKR-CMK peptide

Decanoyl-RVKR-CMK peptide

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

Batch to batch variation of the purity

Decanoyl-RVKR-CMK, Amino terminal decanoyl, acid terminal chlororomethylketone

4

95.28%

C₃₄H₆₆ClN₁₁O₅

744.42

Synthetic

Powder

Decanoyl-RVKR-CMK is a subtilisin/Kex2p-like proprotein convertase inhibitor which blocks the activity of all seven convertases, PC1, PC2, PC4, PACE4, PC5, PC7 and furin. Proprotein convertases are involved in generating bioactive peptides and activating several enzymes and growth factors in many physiological events so have important roles in some pathologies including viral infections and cancer. Decanoyl-RVKR-CMK abolishes proET-1 processing in endothelial cells and inhibits regulated secretion of the neuronal polypeptide VGF. Decanoyl-RVKR-CMK can also inhibit cleavage of the SARS-CoV-2 spike protein by furin and blocks viral cell entry with an IC50 of 57 nM in a plaque reduction assay.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual: Handling and Storage of Synthetic Peptides

• Denault et al (1995) Inhibition of convertase-related processing of proendothelin-1. J.Cardiovasc.Pharmacol. 26 S47 PMID: 8587448
• Fugère and Day (2005) Cutting back on pro-protein convertases: the latest approaches to pharmacological inhibition. Trends Pharmacol Sci. 6 294 PMID: 15925704
• Cheng et al (2020) Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects. Cell Rep. 33 108254 PMID: 33007239

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.