Abstract: Nrf2 is a multi-effect transcription factor, which plays a crucial role in cytoprotective system. With the deepening of research on new regulatory modes and biologic functions of Nrf2, the oncogenic role of Nrf2 in malignant transformed tumors is increasingly obvious. More and more evidences show that Nrf2 is involved in the whole process of tumor occurrence, development, metastasis and prognosis, and inhibiting Nrf2 may be a promising strategy in tumor therapy. However, the development of Nrf2 inhibitors is still in early stage. In this paper, the biological function of Nrf2 and its dual role in tumor are briefly introduced, and representative Nrf2 inhibitors are reviewed according to their structure types, so as to provide reference and ideas for the development of anti-tumor drugs centering on the regulation of Nrf2.