Given its critical role in cancer cell survival, metastasis, and drug resistance, V-ATPase is considered a potential therapeutic target. Inhibitors of V-ATPase, such as Bafilomycin A1 and Concanamycin A, have shown promise in preclinical studies by inducing cancer cell death and enhancing the efficacy of chemotherapy. However, the development of specific and effective V-ATPase inhibitors for clinical use remains challenging.