urokinase

4-Chlorophenylguanidine hydrochloride is a potent and selective inhibitor of urokinase.

Urokinase peptidolytic (Urokinase-type plasminogen activator) is a serine protease, an inactive form (zymogen) of the serine protease plasminogen. Activation of plasmin triggers a proteolytic cascade reaction, which in turn participates in thrombolysis or extracellular matrix degradation, implicated in vascular disease and cancer-related research [1] .

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] [2].

Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).

1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

UKI-1 is a urokinase-type plasminogen activator system synthetic inhibitor.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

ZK824859 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA) with IC50 values of 79 nM for human uPA, 1580 nM for tPA, and 1330 nM for plasmin.

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).

Upamostat, also known as Mesupron and WX-671, is an orally bioavailable second-generation serine protease inhibitor prodrug derived from 3-amidinophenylalanine. It targets the human urokinase plasminogen activator (uPA) system and exhibits potential antineoplastic and antimetastatic properties. After oral administration, the serine protease inhibitor WX-671 is converted into its active form, Nα-(2,4,6-triisopropylphenylsulfonyl)-3-amidinophenylalanine-4-ethoxycarbonylpiperazinylamide (WX-UK1), which inhibits multiple serine proteases, especially uPA, potentially hindering tumor growth and metastasis.

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).

BC 11 hydrobromide is a selective TMPRSS2 and urokinase (uPA) inhibitor.BC-11 induces diminished mitochondrial activity, promotes reactive oxygen species production, and promotes apoptosis, and can be used in the study of breast cancer.

Angstrom6 (A-6 peptide) is an 8 amino acid peptide derived from single chain urokinase fibrinogen activator (scuPA) that interferes with the uPA uPAR cascade and abrogates the downstream effects.Angstrom6 has antitumor activity and inhibits tumor cell migration, invasion, and metastasis by binding to CD44 and modulating CD44-mediated cell signaling.

SSR-182289A (Free) is a thrombin inhibitor.

Chromozym U can be used as a chromogenic substrate test for urokinase in Shigella.

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)

MK-1064 (Urokinase inhibitor 1) is a selective orexin 2 receptor antagonist (2-SORA).

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.

ZK824190 hydrochloride is a selective, orally active urokinase-type fibrinogen activator (uPA) inhibitor that acts on uPA (IC50: 237 nM), tPA (IC50: 1600 nM) and Plasmin (IC50: 1850 nM). hydrochloride can be used in studies of multiple sclerosis

ZK824859 hydrochloride is a selective, orally active inhibitor of urokinase-type fibrinogen activator (uPA) with IC50 values of 79 nM, 1580 nM and 1330 nM for human uPA, tPA and fibrin, respectively.

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.