Biological Information
Background Information:
Urokinase, also called urokinase-type Plasminogen Activator (uPA), is a serine protease. Urokinase was originally isolated from human urine, but is present in several physiological locations, such as blood stream and the extracellular matrix. Urokinase specifically cleaves the proenzyme/zymogen plasminogen to form the active enzyme plasmin. The active plasmin is then able to break down the fibrin polymers of blood clots. This links urokinase to vascular diseases and cancer.
Family:
Protease
Sub Family:
Chymotrypsin
Class:
Serine Peptidase
Protein Name:
Urokinase
Uniprot Number:
P00749
Gene Name:
PLAU
Gene ID:
5328
Gene Aliases:
URK|UPA
Accession Number:
NM_002658
Organism:
Human
Construct Details:
Endogenous
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human urine urokinase is used. Test compound and/or vehicle is preincubated with 1 µg/ml enzyme‡ in modified Tris-HCl buffer pH 7.4 for 15 minutes at 25°C. The reaction is initiated by addition of 100 µM Z-Gly-Gly-Arg-AMC for another 15 minute incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at 360 nm/465 nm. Compounds are screened at 10 µM.
Substrate:
100 µM Z-Gly-Gly-Arg-AMC
Incubation:
15 min at 25°C
Control Inhibitor:
GGACK
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Adverse / Beneficial Action:
Clinically, urokinase is used for the treatment of acute ischemic stroke. Inhibition of urokinase may be anti-inflammatory, reduce tumor invasion and angiogenesis.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei