Lipids, one of the three major nutrients, plays an important role in supplying and storing energy, constructing cells and taking part in cell life activities as an active molecule. One of the most important characteristics of cancer metabolism is the abnormal lipid metabolism, showing the denovo fatty acid synthesis and the active oxidative metabolism, which are closely related to the enhancement of tumor signal transduction pathway and the change of metabolic enzymes. Recently, the related enzymes and transcription factors in the lipid metabolism pathway are potential drug targets for cancer therapy. SREBP-1 is a key transcription factor which regulates the expression of key enzymes in cholesterol or fatty acids synthesis and controls lipogenesis. The expression and activity of SREBP-1 and its regulated fatty acid synthesis pathway are low in normal tissues and cells, while SREBP-1 is activated, accompanying the increase of the downstream gene expression in the tumor cells, which accelerate the synthesis of intracellular fatty acids and cholesterol and regulate lipid metabolism, glucose metabolism and amino acid metabolism via intracellular signaling pathways to provide additional energy and substrates to maintain proliferation and metastasis of tumor cells. The expression and activation of SREBP-1 in tumor cell can be inhibited by genetic and pharmacological means, which significantly suppress the proliferation and migration of tumor cells in vivo and in vitro. Therefore, SREBP-1 has emerged as a promising tumor therapeutic target. In this paper, the effects of abnormal expression of SREBP-1 on tumor signal pathway and metabolism and the development of SREBP-1 inhibitors as anti-cancer agents in cancer were reviewed.