Furin Inhibitor

DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (K_i=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position.

SSM-3 tetraTFA hydrate is a potent furin inhibitor with an EC₅₀ of 54 nM. SSM-3 tetraTFA hydrate uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 tetraTFA hydrate can be used in the research of anthrax and avian influenza.

DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (K_i=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position.

SSM-3 tetraTFA is a potent furin inhibitor with an EC₅₀ of 54 nM. SSM-3 tetraTFA uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 tetraTFA can be used in the research of anthrax and avian influenza.

PAI-1 is a serine protease inhibitor (SERPIN). PAI-1 binds to and irreversibly inhibits uPA, tPA and furin; it also interacts with vitronectin, α1-acid glycoprotein, CRT, TLR4, proteasome α-3 subunit, uPAR, LRP1, Integrin αvβ3 and thrombin. PAI-1 regulates fibrinolysis, extracellular matrix turnover, cell migration, angiogenesis, inflammatory response and tissue remodeling; it mediates epithelial-mesenchymal transition (EMT)/endothelial-mesenchymal transition (EndMT), apoptosis and thrombus stabilization. PAI-1 can be used in research related to sepsis, acute lung injury, cardiovascular diseases, tissue fibrosis, diabetic nephropathy, obstructive nephropathy and non-insulin-dependent diabetes mellitus.

Furin-IN-3 is a non-peptidic furin inhibitor with a dichlorobiphenyl-derived core, with a K_i value of 1.67 nM for furin inhibition and a K_i value of 278 nM for proprotein convertase PC7 inhibition. Furin-IN-3 can be used in the research of influenza A virus infection (H7N7 strain SC35M).

SSM-3 is a potent furin inhibitor with an EC₅₀ of 54 nM. SSM-3 uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 can be used in the research of anthrax and avian influenza.

Furin-IN-2 (compound P3) is a potent inhibitor of furin, with the IC₅₀ of 35 μM. Furin-IN-2 shows antiviral activity.