In certain cancers or pre-cancerous lesions, an increase in the expression of cathepsin B, which is located in lysosomes, is observed. Although Ac-LVK-CHO is currently available and is found to effectively inhibit cathepsin B, it is not able to enter the lysosomes sufficiently to exert its therapeutic effect precisely. In this study, Ac-LVK-CHO was synthesized, and its structure was chemically modified to produce a prodrug aimed at enhancing drug efficacy. Our synthesis method and modifying groups were designed, and a morpholine group was successfully introduced to the amine of Ac-LVK-CHO, allowing it to be more permeable to lysosomes. A photolabile protecting group, 2-nitrobenzyl alcohol, was incorporated at the aldehyde end, enabling the prodrug's activity to be exerted in a controlled manner within lysosomes. The photolabile properties of the prodrug were validated through experiments. Through HPLC chromatograms and mass spectrometry, it was confirmed that this drug can be fully released upon 30 seconds of light exposure, and the photolysis process was determined to follow a first-order reaction. Quantitative data on the prodrug's accumulation in lysosomes will be compiled, and a comprehensive efficacy evaluation of the synthesized prodrug will be completed.