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).
JTV-803 is a factor Xa inhibitor. JTV-803 showed a competitive inhibitory effect on human factor Xa, with a K(i) value of 0.019 microM and IC(50) value of 0.081 microM. JTV-803 was 100 times more selective in inhibiting human factor Xa as compared to its
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.
N-p-Tosyl-Gly-Pro-Lys-pNA is a colorimetric substrate for plasmin.1,2,3Plasmin binds and hydrolyzes N-p-tosyl-Gly-Pro-Lys-pNA to releasep-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of plasmin activity. 1.Jespersen, J., Gram, J., and Astrup, T.The autodigestion of humanplasmin follows a bimolecular mode of reaction subject to product inhibitionThromb. Res.41(3)395-404(1986) 2.Kim, S.H., and Choi, N.S.Electrophoretic analysis of protease inhibitors in fibrin zymographyAnal. Biochem.270(1)179-181(1999) 3.Chen, T., and Rael, E.D.Purification of M5, a fibrinolytic proteinase from Crotalus molossus molossus venom that attacks complementInt. J. Biochem. Cell Biol.29(5)789-799(1997)
p-APMSF is an irreversible inhibitor of serine proteases with Ki values of 1.02, 1.18, 1.5, and 1.54 μM for bovine trypsin, human thrombin, bovine plasmin, and bovine Factor Xa, respectively. It is selective for these proteases over bovine chymotrypsin and acetylcholinesterase.