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Graphene with unique physical and chemical properties has shown various potentialapplications in biomedicine. In this work, a photosensitizer molecule, Chlorin e6 (Ce6), is loaded onpolyethylene glycol (PEG)-functionalized graphene oxide (GO) via supramolecular ππ stacking.The obtained GO-PEG-Ce6 complex shows excellent water solubility and is able to generate cytotoxicsinglet oxygen under light excitation for photodynamic therapy (PDT). Owing to the significantlyenhanced intracellular trafficking of photosensitizers, our GO-PEG-Ce6 complex offers a remarkablyimproved cancer cell photodynamic destruction effect compared to free Ce6. More importantly, weshow that the photothermal effect of graphene can be utilized to promote the delivery of Ce6molecules by mild local heating when exposed to a near-infrared laser at a low power density,further enhancing the PDT efficacy against cancer cells. Our work highlights the promise of usinggraphene for potential multifunctional cancer therapies.