Organelle‐targeting photosensitizers have attracted increasing attention in the development of drugs for photodynamic therapy because they can efficiently induce cellular functional disorder upon light irradiation. In this work, we reported a ruthenium(II) complex bearing two lipophilic carbon chains which specifically binds to the cell membrane. Light irradiation on the complex‐treated cells caused an increase of intracellular reactive oxygen species. The photocytotoxicity of the complex toward HeLa cells were evaluated via the 3‐(4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. A high dose (3 µm) of the complex induced apoptotic cell death by photogeneration of intracellular reactive oxygen species. A low dose (0.25 µm) of the complex did not cause noticeable cell death but increased the permeability of the cell membrane upon light irradiation. [ABSTRACT FROM AUTHOR]