human upa

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.

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].

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.

APC-6860 is a trypsin-like serine protease inhibitor with \( k_i \) values of 0.21, 0.44, 1.5, 16.8, 20, and 30 μM for uPA, trypsin, tryptase, tPA, thrombin, and factor Xa, respectively. It exhibits a selectivity ratio for tPA versus uPA of 80 and has \( k_i \) values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be utilized for cancer research.

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.

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.

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.