The cation cis-[Ru(bpy)(2)(SCNU)(2)](2+) (bpy = 2,2'-bipyridine; SCNU = S-cyanouracil) was synthesized and investigated for use as a potential light-activated dual-action therapeutic agent. The complex undergoes efficient photoinduced SCNU ligand exchange for solvent water molecules, thus simultaneously releasing biologically active SCNU and generating [Ru(bpy)(2)(H2O)(2)](2+). The latter binds covalently to ds-DNA, such that photolysis results in the generation of 3 equiv of potential therapeutic agents from a single molecule.