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] .

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

4-Chlorophenylguanidine hydrochloride is a potent inhibitor of urokinase selectivity.

Cenupatide acetate is an urokinase plasminogen activator receptor (uPAR) inhibitor for treating disorders associated altered cell migration, such as cancer.

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.

Cenupatide is a urokinase plasminogen activator receptor (uPAR) inhibitor. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of STZ-induced diabetes. Cenupatide reverted STZ-induced up-regula

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.

Plasminogen is a zymogen secreted as a precursor protein that, when cleaved by urokinase plasminogen activator (uPA) or tissue plasminogen activator (tPA), is converted into plasmin. Plasmin is a protease with broad specificity, capable of degrading fibrin and various extracellular matrix (ECM) components. Additionally, plasminogen functions as a proinflammatory regulator, promoting the healing of both acute and diabetic wounds. It is utilized in research related to wound healing, inflammation, and hypoplasminogenemia [1] [2].

Vitronectin, a multifunctional glycoprotein found in blood and the extracellular matrix, interacts with glycosaminoglycans, collagen, plasminogen, and the urokinase-receptor, in addition to stabilizing the inhibitory conformation of plasminogen activation inhibitor-1. It is utilized in research related to wound healing and tumor progression [1].

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA) as a potential treatment for multiple sclerosis(IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively).

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).

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].

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.

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)

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

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).

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.

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

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.

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).

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

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.

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.

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

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

UCD74A HCl is a cell impermeant homolog of UCD38B, inhibitor of uPA (urokinase plasminogen activator).