uPA Inhibitor II, UK122 is a cell-permeable oxazolidinone-carboxamidine compound reported to act as a potent, selective, and active-site targeting urokinase-type plasminogen activator (uPA, IC50 = 200 nM) inhibitor. Its activity against trypsin, thrombin, tPA, and plasmin, however, is greatly reduced. Additionally, uPA Inhibitor II, UK122 has been reported to effectively inhibit the migration (80% inhibition) and invasion (68% inhibition) of uPA-expressing CFPAC-1 pancreatic cells, without affecting the proliferation of these cells.
1. Zhu, Ming., et al., 2007. Identification of a novel inhibitor of urokinase-type plasminogen activator. Molecular cancer therapeutics. 6(4): 1348-56. PMID: 17431113
Rated 1 out of
Useless in cell cultureWhile it is an efficient inhibitor in HEPES buffer it is not able to inhibit urokinase in a tissue culture medium. Easy to check!
Date published: 2017-12-07
Rated 5 out of
ChoCho, E. et al. (PubMed 22293605) reported that uPA renders neurons resistant to kainate-induced excitotoxicity. When they applied UK122 these neuroprotective effects were diminished. -SCBT Publication Review
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