Biological Information

Background Information:

Phospholipase A2 (PLA2) catalyzes the release of arachidonic acid from phospholipids and is important in the formation of inflammatory mediators. Secretory PLA2, divided into three groups, are the most highly characterized group of PLA2 enzymes due to its ubiquitous nature and high concentration in pancreatic juices and venoms of snakes. Group II PLA2 (PLA2-II) is found in rheumatoid synovial fluid and in plasma after inflammatory challenge. Increase serum levels of PLA2-II have been demonstrated in patients with ulcerative colitis and septic shock.

Family:

Lipid Metabolism

Sub Family:

Glycerophospholipid Turnover

Class:

Phospholipase A2

Protein Name:

PLA2G2A

Uniprot Number:

P14555

Protein Aliases:

GIIC sPLA2; Group IIA phospholipase A2;Non-pancreatic secretory phospholipase A2 (NPS-PLA2);Phosphatidylcholine 2-acylhydrolase 2A

Gene Name:

PLA2G2A

Gene ID:

5320

Gene Aliases:

PLA2B;PLA2L

Accession Number:

NM_000300

Organism:

Human

Construct Details:

Fragment, recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant phospholipase A2 group IIA (PLA2G2A) expressed in Sf21 cell line is used. Test compound and/or vehicle is preincubated with 25 ng/ml enzyme in modified Tris-HCl buffer at pH 8.5 for 15 minutes at 25˚C. The reaction is initiated by addition of 20 µM β-py-C10-PG for another 10-minute incubation period. Determination of the amount of 10-pyrenyldecanoic acid formed is read spectrofluorimetrically at Excitation: 342 nm; Emission: 395 nm. Compounds are screened at 10 μM.

Substrate:

20 µM β-py-C10-PG

Incubation:

10 min at 25°C

Control Inhibitor:

Varespladib

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

9853400

Name

YM 26734

Measurement

1.8μM - IC50

PubChem ID

155922

Name

LY311727

Measurement

0.65μM - IC50

PubChem ID

129909859

Name

AZD 2716

Measurement

0.51μM - IC50

PubChem ID

446400

Name

sPLA2 inhibitor 1

Measurement

0.7μM - IC50

PubChem ID

155815

Name

Varespladib

Measurement

0.072μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei