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.

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.

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).

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