Isoscopoletin is a hydroxycoumarin that is esculetin in which the hydroxy group at position 7 is replaced by a methoxy group. It is the major primary metabolite of scoparone. It has a role as a plant metabolite. It is an aromatic ether and a hydroxycoumarin. It is functionally related to an esculetin. Isoscopoletin possesses inhibitory activity against hepatitis B virus (HBV) replication; it also shows substantial inhibition against multi-drug resistant CEM/ADR5000 cells and human CCRF-CEM leukaemia cells, with the IC50 value is 1.6 and 4.0 microM, respectively.