Plasminogen activator inhibitor-1 (PAI-1) inhibitor. Inhibits VEGF-induced migration and tube formation in HUVECs. Also attenuates TGF-β dependent epithelial-mesenchymal transition and fibroblast to myofibroblast differentiation in vitro. Reduces size and weight of subcutaneous tumors, and inhibits metastasis and angiogenesis in vivo. Reduces bleomycin-induced pulmonary fibrosis in vivo. Orally bioavailable.

Omori et al (2016) Inhibition of plasminogen activator inhibitor-1 attenuates transforming growth factor-β-dependent epithelial mesenchymal transition and differentiation of fibroblasts to myofibroblasts. PLoS One. 11 e0148969 PMID:26859294 |Takayama et al (2016) Inhibition of PAI-1 limits tumor angiogenesis regardless of angiogenic stimuli in malignant pleural mesothelioma. Cancer Res. 76 3285 PMID:27197170 |Masuda et al (2013) SK-216, an inhibitor of plasminogen activator inhibitor-1, limits tumor progression and angiogenesis. Mol.Cancer Ther. 12 2378 PMID:23990114