urokinase-type ,plasminogen

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

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

GGACK (H-Glu-Gly-Arg-CMK) hydrochloride is an irreversible substrate-like inhibitor of the serine protease urokinase-type plasminogen activator (uPA).

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.

Amiloride (MK-870) is an inhibitor of the epithelial sodium channel (ENaC) and the urokinase-type plasminogen activator receptor (uPAR). It also acts as a blocker of the polycystin-2 (PC2; TRPP2) channel.

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.

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.

Urokinase peptidolytic,Urokinase-type plasminogen activator (uPA) is a trypsin-like serine protease that exists as an inactive zymogen (pro-uPA) and requires proteolytic cleavage for its activation. once activated, it serves as the central catalyst in a proteolytic cascade that converts plasminogen to plasmin, a process critically involved in physiological and pathological thrombolysis and extracellular matrix degradation.

Bicyclic UK18 is a competitive inhibitor of human urokinase-type plasminogen activator (uPA) with a Ki value of 53 nM.

UK140 is an inhibitor of the urokinase-type plasminogen activator (uPA), with Ki values of 0.20 µM for human uPA (huPA) and 2.79 µM for mouse uPA (muPA). UK140 is applicable in studies related to tumor metastasis.

GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like inhibitor of the serine protease urokinase-type plasminogen activator (uPA).

SA-21 is a polymeric peptide consisting of 21 amino acids (Ac-RLIEDICLPRWGCLWEDD-NH2) capable of binding to the ligand of urokinase-type plasminogen activator, Fab antibody fragments, and small proteins. It is useful for purifying albumin (Ki=1.9 μM).

E16-uPA24 is a chimeric peptide that targets the urokinase-type plasminogen activator receptor (uPAR). It uses polyglutamic acid to modify the surface of senescent cells, promoting an immune response through glutamic acid recognition. This compound enhances immune cell recruitment and directly links senescent and immune cells, leading to the immune clearance of senescent cells and the restoration of tissue homeostasis. E16-uPA24 is applicable in research on tissue degeneration, chronic inflammatory diseases, and age-associated tumorigenesis.