Biological Information
Background Information:
The major neutral proteases of neutrophil granules are the serine proteases elastase and cathepsin G, a serine protease. The latter enzyme shows a strong preference for hydrophobic substrates. Since these enzymes degrade connective tissue and other proteins, inhibition of either one or both enzymes may be therapeutically beneficial in pathological conditions where neutrophils are implicated. Inhibitors of these enzymes are potentially useful for the treatment of rheumatoid arthritis, psoriasis, periodontitis and other inflammatory diseases.
Family:
Protease
Sub Family:
Chymotrypsin
Class:
Serine Peptidase
Protein Name:
Cathepsin G
Uniprot Number:
P08311
Gene Name:
CTSG
Gene ID:
1511
Gene Aliases:
CG
Accession Number:
NM_001911
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 neutrophil cathepsin G is used. Test compound and/or vehicle is preincubated with 25 ug/ml enzyme‡ in modified acetate buffer pH 5.5 for 15 minutes at 25⁰C. The reaction is initiated by addition of and 20 μM Suc-Ala-Ala-Pro-Phe-AMC for another 30 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:
20 µM Suc-Ala-Ala-Pro-Phe-AMC
Incubation:
30 min at 25°C
Control Inhibitor:
Chymostatin
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
Therapeutic Area:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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