decanoyl-RVKR-chloromethyl ketone

Decanoyl-RVKR-chloromethyl ketone (also known as Furin Inhibitor I or dec-RVKR-cmk) is a cell-permeable, irreversible, broad-spectrum inhibitor of proprotein convertases (PCs). It specifically targets the subtilisin/Kex2p-like proprotein convertases, including Furin (PCSK3), PC1/3 (PCSK1), PC2 (PCSK2), PC4 (PCSK4), PACE4 (PCSK6), PC5/6 (PCSK5), and PC7 (PCSK7). The compound consists of a decanoyl fatty acid chain that facilitates membrane permeability, a peptide sequence (Arg-Val-Lys-Arg) mimicking the consensus recognition site of PCs, and a chloromethyl ketone (CMK) warhead that covalently binds to the active site histidine residue of the target enzymes. It is widely used as a research tool to study the proteolytic processing of precursor proteins, such as viral glycoproteins (e.g., SARS-CoV-2 spike protein, HIV-1 gp160, and RSV fusion protein) and growth factors involved in cancer progression. While it has shown preclinical potential in inhibiting viral entry and suppressing cancer stem cell properties, it is a research tool compound and is not in clinical development for human use.

Other names

Furin Inhibitor IDec-Arg-Val-Lys-Arg-CMKDec-RVKR-CMKCAS 150113-99-8CAS150113-99-8CAS-150113-99-8