VD4162 (Compound 8b) is a macrocyclic inhibitor of serine proteases. VD4162 can significantly improve potency for all four target enzymes TMPRSS2 ( IC 50 = 3.7 nM), HGFA( IC 50 = 3.3 nM), matriptase ( IC 50 = 2.9 nM), and hepsin ( IC 50 = 0.54 nM). VD4162 can be used for the research of cancer.