ZK824859 is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
ZK824859 hydrochloride is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (2700-fold versus plasmin and 4000-fold versus tPA).
PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.
GGACK is an inhibitor of urokinase-type plasminogen activator (uPA) and factor Xa (Kis = 1.8 and 8.7 μM, respectively).1,2 1.Kettner, C., and Shaw, E.The susceptibility of urokinase to affinity labeling by peptides of arginine chloromethyl ketoneBiochim. Biophys. Acta569(1)31-40(1979) 2.Kettner, C., and Shaw, E.The selective affinity labeling of factor Xa by peptides of arginine chloromethyl ketoneThromb. Res.22(5-6)645-652(1981)
UK122 is a highly effective and specific inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 0.2 μM. It displays negligible to minimal inhibition towards tissue-type plasminogen activator (tPA), plasmin, thrombin, and trypsin (all IC50 >100 μM). Functioning as a 4-oxazolidinone analogue, UK122 is an anticancer agent that effectively inhibits cancer cell migration and invasion.
CJ-463 is a potent ans selective uPA inhibitor. Treatment with CJ-463 resulted in a significant inhibition of primary tumor growth, with the highest efficacy seen in the 100 mg kg group. Urokinase (uPA) plays a crucial role in carcinogenesis by facilitating tumor cell invasion and metastasis. CJ-463 may be a novel agent for treatment of lung cancer.
UK-356,202 is a potent and selective urokinase-type plasminogen activator (Ki = 37 nM). Urokinase plasminogen activator (uPA, urokinase) is a trypsinlike serine protease and a therapeutical target for many cancer types, including breast, ovarian, and pancreatic cancer. uPA is a valuable oncology target.