ABSTRACT: Traditional Chinese medicines have a long history of clinical application. However, their therapeutic mechanisms are still largely unknown. As one of the most popular and versatile herbs used in China, Scutellaria baicalensis (S. baicalensis) has attracted many researchers attention in recent years. Studies revealed that the herb possesses numerous bioactivities, including antitumor, antiallergic, neuroprotective, anti-inflammatory, cardiovascular protective, hepatoprotective, antiviral and antibacterial activities. This review summarizes current knowledge about bioactive components, bioactivities and therapeutic potential of S. baicalensis based on latest literature, aiming to provide insights for further study and application of this famous herbal medicine.