Salvia miltiorrhiza Bunge (Danshen in Chinese) is a classical Huoxue Huayu (a traditional Chinese medical term means promoting blood circulation and removing blood stasis) herb with 1000 years of clinical application. It mainly contains two groups of ingredients: the hydrophilic phenolic acids and the lipophilic tanshinones. Both groups have demonstrated multiple bioactivities, such as antioxidative stress, antiplatelet aggregation, anti-inflammation, among others. Recent data have demonstrated that its lipophilic compounds, especially the tanshinones, show potent anticancer activities both in vitro and in vivo. The anticancer effects of the hydrophilic phenolic acids have also been reported. Furthermore, tanshinones provide structural skeletons for chemical modifications, allowing for a series of derivatives of interests. This review provides a systematic summary of the anticancer profile and the underlying mechanisms of the bioactive compounds isolated from Danshen with special emphasis on tanshinones, aiming to bring new insights for further research and development of this ancient herb.