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

PubChem ID

57352181

Name

GGACK

Measurement

0.067μM - IC50

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