Excimer Emission-Based Fluorescent Probe Targeting Caspase-3

A fluorescent probe based on an excimer-forming benzothiazolyl-cyanovinylene (CV) dye was developed to target the apoptotic protease caspase-3. Upon the action of caspase-3, the water-soluble fluorescent probe Ac-DEVD-NH-CV, which is weakly green emissive in aqueous solution, is converted to hydrophobic CV-NH2, which spontaneously aggregates. Aggregation of CV-NH2 promotes excimer emission of the CV dye, which allows for the study of caspase-3 activity in vitro and for imaging the activity of the enzyme in living cells because of the large red shift and enhanced fluorescence signal of the probe.