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

PubChem ID

132519

Name

Ilomastat

Measurement

0.00086μM - IC50

PubChem ID

135316240

Name

TIMP-2

Measurement

0.004μM - IC50

PubChem ID

Name

TIMP-1

Measurement

0.0039μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP258