Subtle ligand modificationso nR u II-polypyridyl complexesm ay result in different excited-state characteristics, which provides the opportunity to tune their photophysicochemical properties and subsequently change their biological functions. Here, aD NA-targeting Ru II-polypyridyl complex (named Ru1)w ith highly photosensitizing 3 IL (intraligand) excited state was designedb ased on ac lassical DNA-intercalator [Ru(bpy) 2 (dppz)]•2PF 6 by incorporation of the dppz (dipyrido[3,2-a:2',3'-c]phenazine) ligand tethered with ap yrenyl group, which hasf our orders of magnitude higher potencyt han the model complex [Ru(bpy) 2 (dppz)]•2PF 6 upon light irradiation. This study provides af acile strategy for the design of organelle-targeting Ru II-polypyridyl complexesw ith dramatically improved photobiological activity.