The main directions and potential obstacles in the regulating mechanism research and therapeutic agents development targeting the cGAS–STING signaling pathway in inflammatory diseases and cancers will be discussed, which will provide a theoretical and practical basis for further study on the precise triggers and regulating mechanisms of cGAS–STING signaling pathway in physiological and pathological conditions, and developing effective drugs with fewer side effects targeting cGAS–STING signaling pathway for the inflammation‐related diseases treatment, especially cancers. Here, STING1 is linked to inflammation.