A new red-emissive bioprobe TPE-red-2AP2H was developed by taking advantage of the unique emission feature of tetraphenylethylene and a cancer cell-specific peptide. By responding to the target protein and the acidic microenvironment of tumor cells, activated fluorescence bioimaging was achieved with high signal-to-noise ratio and without involving mutiple washing steps. Apart from targeting the membrane-anchored LAPTM4B proteins, TPE-red-2AP2H was successfully utilized to trace the intracellular movement of LAPTM4B protein. The generation of 1O2 under visible light irradiation makes this bioprobe also promising for targeted-photodynamic therapy. By discriminating the expression level of the target protein, TPE-red-2AP2H can respond to the progression status of tumors with different photodynamic therapy effect.