In the present study, for the first time, we demonstrated that IMD-4482 significantly reduced uPAR/αVβ3 integrin-mediated adhesion to VN, followed by the reduction of FAK and ERK phosphorylation and inhibition of cell proliferation as a result of G0/G1 arrest, leading to a novel rationale that inhibition of PAI-1 can be a potential therapy for ovarian cancer. This evidence concerns the gene SERPINE1 and ovarian cancer.