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Products
Pharmacology
Type
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- Custom services
- Ordering
- About Us
- Technical support
- Resources
Decanoyl-RVKR-CMK
Cat. No. OP-010
Structure:
Decanoyl-Arg-Val-Lys-Arg-CMK
Other Names:
dec-RVKR-cmk, Furin Inhibitor I, decanoyl-RVKR-chloromethylketone,
Activity:
Proprotein convertase inhibitor
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.
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
Related areas
All peptides >
All other protease modulators >
All antivirals >
Technical Data
| Structure | Decanoyl-Arg-Val-Lys-Arg-CMK |
| CAS Number | 150113-99-8 |
| Molecular Weight | 744.42 |
| Formula | C34H66ClN11O5 |
| Sequence | Decanoyl-RVKR-CMK |
| Modifications | Amino terminal decanoyl, acid terminal chlororomethylketone |
Solubility and Storage
| Solubility | Soluble to 1 mg/ml in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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