Two orally available small molecule anti-PAI-1 agents, TM5441 and TM5275, inhibited the proliferation of different types of cancer cell lines (MDA-MB-231 (breast cancer), HCT116 (colorectal cancer), HT1080 (fibrosarcoma), Jurkat (acute T cell leukemia), Daoy (medulloblastoma)) with an IC50 range between 9.7 and 60.3 μM [128]. The gene discussed is SERPINE1; the disease is cancer.