In　this　study,　we　demonstrate　a　novel　H2O2　activatable　photosensitizer　(compound　7)　which　contains　a　diiodo　distyryl　boron　dipyrromethene　(BODIPY)　core　and　an　arylboronate　group　that　quenches　the　excited　state　of　the　BODIPY　dye　by　photoinduced　electron　transfer　(PET).　The　BODIPY-based　photosensitizer　is　highly　soluble　and　remains　nonaggregated　in　dimethyl　sulfoxide　(DMSO)　as　shown　by　the　intense　and　sharp　Q-band　absorption　(707　nm).　As　expected,　compound　7　exhibits　negligible　fluorescence　emission　and　singlet　oxygen　generation　efficiency.　However,　upon　interaction　with　H2O2,　both　the　fluorescence　emission　and　singlet　oxygen　production　of　the　photosensitizer　can　be　restored　in　phosphate　buffered　saline　(PBS)　solution　and　PBS　buffer　solution　containing　20%　DMSO　as　a　result　of　the　cleavage　of　the　arylboronate　group.　Due　to　the　higher　concentration　of　H2O2　in　cancer　cells,　compound　7　even　with　low　concentration　is　particularly　sensitive　to　human　cervical　carcinoma　(HeLa)　cells　(IC50　=　0.95　M)　but　hardly　damage　human　embryonic　lung　fibroblast　(HELF)　cells.　The　results　above　suggest　that　this　novel　BODIPY　derivative　is　a　promising　candidate　for　fluorescence　imaging-guided　photodynamic　cancer　therapy.