Dimethylacrylshikonin usually can be found in the roots of Lithosperraum erythrorhizon Sieb. et Zucc. Injection of Dimethylacrylshikonin combined with IR treatment significantly suppressed tumor growth of the HCT-116 xenograft. Dimethylacrylshikonin is a promising agent for developing an improved strategy for radiotherapy against tumors. Dimethylacrylshikonin is a potent inhibitor of progression of gastric cancer cells, which could be due to attenuation of Notch-1. Dimethylacrylshikonin inhibits the proliferation of MCF-7 cells in vitro by inducing apoptosis through the downregulation of Bcl-2, upregulation of Bax and partial inactivation of the NF-κB pathway.