Furin Inhibitor I (trifluoroacetate salt)

Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LPC/PC7/PC8 (Ki = 0.12 nM).1,2 Because furin activates viral glycoproteins, this inhibitor is a useful antiviral agent.3 In addition, it inhibits furin-dependent pro-MMP-2 activation in mononuclear inflammatory cells.4WARNING This product is not for human or veterinary use.

[1] H ANGLIKER. The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast.[J]. Biochemical Journal, 1993, 293 ( Pt 1): 75-81. DOI: 10.1042/bj2930075
[2] M. FUGÈRE. Inhibitory Potency and Specificity of Subtilase-like Pro-protein Convertase (SPC) Prodomains*[J]. The Journal of Biological Chemistry, 2002, 14 1: 7648-7656. DOI: 10.1074/jbc.m107467200
[3] JANE W WANYIRI. Proteolytic processing of the Cryptosporidium glycoprotein gp40/15 by human furin and by a parasite-derived furin-like protease activity.[J]. Infection and Immunity, 2007: 184-192. DOI: 10.1128/iai.00944-06
[4] PHILIPP STAWOWY. Furin-like proprotein convertases are central regulators of the membrane type matrix metalloproteinase-pro-matrix metalloproteinase-2 proteolytic cascade in atherosclerosis.[J]. Circulation, 2005, 111 21: 2820-2827. DOI: 10.1161/circulationaha.104.502617