Osteosarcoma is a malignant tumor that histologi- cally forms a tumor-like osteoid or bone. Plasmino- gen activator inhibitor 1 (PAI-1) is highly expressed in the blood of patients with various malignant tumors or in the tumors themselves, and its expres- sion is positively correlated with tumor grade. Therefore, PAI-1 is a potential target for cancer therapy. In this study, a small-molecule PAI-1 inhib- itor, TM5614, was tested on U2OS cells, which are osteosarcoma cell-like cells, to examine its effect on cell metabolism. The MTT assays and cell count analysis showed that TM5614 inhibited U2OS cell proliferation. We also tested the apoptotic activity of U2OS cells by multiple assays, and no induction of apoptosis by TM5614 was observed. In contrast, cell cycle analysis revealed that TM5614 induced U2OS cells in G2-M arrest. This study revealed that TM5614 treatment increased p53 and p21 Waf1/Cip1 expression in U2OS cells. In conclusion, we showed that the PAI-1 inhibitor TM5614 induced G2-M arrest in U2OS cells.

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