Decanoyl-RVKR-CMK

Biological Activity

Decanoyl-RVKR-CMK is a subtilisin/Kex2p-like proprotein convertase inhibitor; blocks activity of all seven convertases (PC1, PC2, PC4, PACE4, PC5, PC7 and furin). Abolishes proET-1 processing in endothelial cells; inhibits regulated secretion of the neuronal polypeptide VGF in PC12 cells. Inhibits cleavage of glycoprotein B of human cytomegalovirus. Also inhibits cleavage of SARS-CoV-2 spike protein by furin and blocks viral cell entry (IC₅₀ = 57 nM in plaque reduction assay).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Cutting Edge: ERK1 Mediates the Autocrine Positive Feedback Loop of TGF-? and Furin in Glioma-Initiating Cells
   E Ventura, M Weller, I Burghardt
   J. Immunol., 2017;0(0):.
2. A prohormone convertase cleavage site within a predicted alpha-helix mediates sorting of the neuronal and endocrine polypeptide VGF into the regulated secretory pathway.
   Garcia et al.
   J.Biol.Chem., 2005;280:41595
3. Comparative study of the binding pocket of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors.
   Tian and Jianhua
   Int.J.Biol.Sci., 2010;6:89
4. Inhibition of convertase-related processing of proendothelin-1.
   Denault et al.
   J.Cardiovasc.Pharmacol., 1995;26:S47
5. Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects.
   Cheng et al.
   Cell Rep., 2020;

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