ZFH7116

ZFH7116 is an acyclic peptide-based small molecule inhibitor of hepatocyte growth factor (HGF)-activating serine proteases, specifically matriptase and hepsin. It was developed as a tool compound and reference inhibitor in the study of HGF/MET signaling pathways. By preventing the proteolytic cleavage of inactive pro-HGF into its active form, ZFH7116 inhibits the activation of the MET receptor tyrosine kinase. In preclinical studies involving lung cancer models, ZFH7116 has been shown to block HGF-mediated cellular processes and restore sensitivity to EGFR and MET inhibitors in resistant cell lines. It serves as a linear precursor or reference compound in the development of more metabolically stable macrocyclic inhibitors like VD2173.