Benzamidine and its derivatives serve as inhibitors of serine protease enzymes, namely tryptase, thrombin, and KLK11 (tripsin-like enzymes). The strong affinity of benzamidine for these enzymes has been exploited to crystallize and study spectra of thrombin complexes. Benzamidine inhibits the autoactivation of human blood coagulation factor VII, useful as a tool for studying the interactions between this and other relevant growth factors. A derivative of this compound has shown activity against the growth of colon cancer cells.
