The genus Schefflera (Araliaceae) consists of 1100 species, 35 of which can be found in China. Some species of the genus have been used in traditional medicine to treat rheumatalgia, trauma, fracture, headache, and so on. Phytochemical studies of the genus have demonstrated the presence of large number of triterpenoids and their saponins, along with some long-chain compounds, steroids and sesquiterpenes. Furthermore, many pharmacological activities of the genus such as anti-inflammatory, anticancer and antiviral activities have been reported. In this article, new development of constituents and biological activities of Schefflera genus is reviewed and summarized for its further development and utilization.