Cancer is a serious disease that endangers human health. Solid tumors are surrounded by extracellular matrix, infiltrated immune cells, and the secretum of surrounding mesenchymal cells. The tumor microenvironment plays a key role in tumorigenesis, tumor growth, and resistance to antineoplastic therapy. Plasminogen activator inhibitor-1 (PAI-1) is an important regulatory factor in tumor microenvironment. PAI-1 not only functions as a key constitution with tissue-type plasminogen activators (tPA) in regulating fibrinolytic activity, but also participates in invasion, infiltration and migration of tumor. In this paper, the structure and function of PAI-1 and its significance in tumor microenvironment in recent years are reviewed. It is considered that PAI-1 may be an important target for anti-cancer therapy. At the same time, the latest research results of PAI-1 inhibitors in the field of anticancer were analyzed, and the potential application value of PAI-1 inhibitors was demonstrated.