Carboxypeptidase G2 inhibitors are primarily used in the field of cancer treatment, particularly in the context of antibody-directed enzyme prodrug therapy (ADEPT). In ADEPT, Carboxypeptidase G2 (CPG2) is employed to activate prodrugs into their cytotoxic forms at tumor sites. However, to control the timing and extent of prodrug activation, CPG2 inhibitors are utilized to modulate the enzyme's activity. This ensures that the cytotoxic effect is localized to the tumor, minimizing damage to healthy tissues. Additionally, these inhibitors are studied for their potential to enhance the precision and efficacy of targeted cancer therapies, reducing systemic toxicity and improving patient outcomes.