SK-216, a specific PAI-1 inhibitor, reduces tumor angiogenesis and inhibits VEGF-induced migration and tube formation of human umbilical vein endothelial cells in vitro. This compound also alleviates bleomycin-induced pulmonary fibrosis in mice.

Methods: Human osteosarcoma cell line 143B was treated with SK-216 (0-50 μM, hours), and the expression of target proteins was detected by Western blot. Results: SK-216 at concentrations of 25 and 50 μM inhibited PAI-1 expression by 40%, resulting in a significant decrease in the ratio of cell invasion pores to total pores, and was able to inhibit the secretion of MMP-13 in 143B cells. [2]

Methods: SK-216 (6.6 μg/200 μL, intraperitoneal injection, once every three days) was used to treat a mouse model of spontaneous lung metastasis to examine whether it inhibits the lung metastasis of human osteosarcoma cells. Results: SK-216 inhibited the lung metastasis of human osteosarcoma cells from the primary lesion, but did not inhibit tumor growth. [2]