UK-122, formerly known as uPA Inhibitor II, is a potent and selective uPA inhibitor (Ki = 20 nM). The IC(50) of UK122 in a cell-free indirect uPA assay is 0.2 micromol/L. UK-122 also showed no or little inhibition of other serine proteases such as thrombin, trypsin, plasmin, and the tissue-type plasminogen activator, indicating its high specificity against uPA. Moreover, UK122 showed little cytotoxicity against CFPAC-1 cells (IC(50) >100 micromol/L) but significantly inhibited the migration and invasion of this pancreatic cancer cell line. UK122 could potentially be developed as a new anticancer agent that prevents the invasion and metastasis of pancreatic cancer. References: Banyard J, Chung I, Migliozzi M, Phan DT, Wilson AM, Zetter BR, Bielenberg DR. Identification of genes regulating migration and invasion using a new model of metastatic prostate cancer. BMC Cancer. 2014 May 30;14:387. doi: 10.1186/1471-2407-14-387. PubMed PMID: 24885350; PubMed Central PMCID: PMC4046438.
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CAS:940290-58-4