Hinokitiol is a natural bioactive compound found in several aromatic and medicinal plants. It is a terpenoid synthetized and secreted by different species as secondary metabolites. This volatile compound was tested and explored for its different biological properties. In this review, we report the pharmacological properties of hinokitiol by focusing mainly on its anticancer mechanisms. Indeed, it can block cell transformation at different levels by its action on the cell cycle, apoptosis, autophagy via inhibiting gene expression and dysregulating cellular signaling pathways. Moreover, hinokitiol also exhibits other pharmacological properties, including antidiabetic, anti-inflammatory, and antimicrobial effects. It showed multiple and several effects through its inhibition, interaction and/or activation of the main cellular targets inducing these pathologies.