BB-Cl-Amidine

BB-Cl-Amidine is a pan-peptidylarginine deiminase (PAD) inhibitor. Peptidylarginine deiminase catalyzes the hydrolysis of peptidyl-arginine to form peptidyl-citrulline. BB-Cl-Amidine is a derivative of the PAD inhibitor Cl-amidine in which the C-terminal carboxamide is replaced with a benzimidazole moiety to reduce proteolysis. The cellular potency of BB-Cl-amidine is 20-fold higher than Cl-amidine. The EC₅₀ value for inhibition of viability of U2OS osteosarcoma cells is 8.8 μM. It improves endothelium-dependent vasorelaxation in MRL/lpr mice. It inhibits the formation of neutrophil extracellular traps without altering H₂O₂ production by neutrophils.