Abstract: In this paper, the research on the discovery, synthesis, biological activities, mechanism of action, non-target toxicity and derivatives of hinokitiol was reviewed. Hinokitiol is a kind of plant secondary metabolite with antimicrobial, insecticidal, anti-inflammatory, anticancer and other biological activities. It can be synthsized from readily available raw materials in industry and has significant development value. The seven-membered ring and carbonyl group of hinokitiol are essential groups for its bioactivity, and the structure-activity relationship suggests that the modification of hydroxyl group position may be one of the important ways to discover the highly active hinokitiol derivatives. However, the action characters, non-target toxicity and structural stability of hinokitiol are still unclear, which greatly limits the application of hinokitiol.