Biological Information
Background Information:
The MMP family shares significant sequence homology and a common multidomain structure. On the basis of their preferred substrates, they can be divided into four main classes: collagenases, gelatinases, stromelysins and membrane-type MMPs. These enzymes demonstrate very low activity in normal tissue but are upregulated and/or activated during inflammation and physiological remodeling processes in response to specific stimuli, including cytokines, growth factors and extracellular matrix interactions. Inhibitors may be useful for cancer, rheumatoid arthritis, autoimmune diseases, periodontitis, tissue ulcerlation, atherosclerosis, aneurysm and heart failure.
Family:
Protease
Sub Family:
Matrix Metallopeptidase
Class:
Metallo Peptidase
Protein Name:
MMP8
Uniprot Number:
P22894
Gene Name:
MMP8
Gene ID:
4317
Accession Number:
NM_002424
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human neutrophil MMP-8 proenzyme, activated with APMA for 60 minutes at 37°C, is used. Test compound and/or vehicle is preincubated with 6.7 nM active enzyme‡ in modified MOPS buffer pH 7.2 for 60 minutes at 37°C. The reaction is initiated by addition of 4 μM Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg for another 120 minute incubation period. Determination of the amount of Mca-Pro-Leu-Gly formed is read spectrofluorimetrically at 340 nm/400 nm. Compounds are screened at 10 μM.
Substrate:
4 µM Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH₂
Incubation:
120 min at 37°C
Control Inhibitor:
GM-6001
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:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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