Abstract: The innate immune response acts as the first line of defense for the host against pathogen invasion. Throughout the process, the cyclic GMP-AMP synthase (cGAS) / stimulator of interferon gene (STING) pathway plays a central role. This pathway not only recognizes double-stranded DNA in the cytoplasm, thus triggering the innate immune response, but also has a close association with antitumor immunity, the aging process, neurodegenerative diseases, and the development of autoimmune diseases. This review summarizes the research progress of STING regulators in recent years, as well as their application in anti-tumor therapies and treatment of autoimmune diseases; it also explores the application prospects of STING regulators in delaying aging, treating neurodegenerative diseases, and serving as vaccine adjuvants, aiming to provide some reference for the research and development of drugs targeting STING.