Biological Information

Background Information:

Humans have six elastase genes which encode the structurally similar proteins elastase 1, 2, 2A, 2B, 3A, and 3B. Neurophil elastase 2 (PMN elastase, Leukocyte elastase, Bone marrow serine protease, Medullasin) is a serine protease that hydrolyzes proteins within specialized neutrophil lysosomes, called azurophil granules, as well as proteins of the extracellular matrix following the protein's release from activated neutrophils. Elastase 2 may play a role in degenerative and inflammatory diseases by its proteolysis of collagen-IV and elastin of the extracellular matrix.

Family:

Protease

Sub Family:

Chymotrypsin

Class:

Serine Peptidase

Protein Name:

Neutrophil Elastase

Uniprot Number:

P08246

Protein Aliases:

neutrophil elastase|leukocyte elastase|medullasin

Gene Name:

ELANE

Gene ID:

1991

Gene Aliases:

NE|HNE|HLE

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrophotometric

Testing Information

Substrate:

MeOSAAPV-pNa (0.4 mM)

Incubation:

30 min at 37°C

Control Inhibitor:

3',4'dichloroisocoumarin

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

4784

Name

Phenylmethylsulfonyl fluoride

Measurement

220000nM - IC50

PubChem ID

24278386

Name

3',4'dichloroisocoumarin

Measurement

395nM - IC50

PubChem ID

2372872

Name

BAY-678

Measurement

455nM - IC50

PubChem ID

57654453

Name

Nordihydroguaiaretic acid

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Inhibition of elastase 2 may be useful in the treatment of degenerative and inflammatory diseases including emphysema, rheumatoid arthritis and psoriasis.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault