Biological Information
Background Information:
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (ENPP 2), also known as autotaxin, is produced as a pre-proenzyme glycoprotein and activated by the removal of its N-terminal signal peptide resulting in a matured secreted form, consists of 4 domains, two N‐terminal SMB‐like domains, a central catalytic PDE domain, and an inactive nuclease‐like domain. ENPP2 acts as a lysophospholipase D, mainly hydrolyzing extracellular lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA). LPA, like a growth factor in serum, could induce motility in fibroblasts and cancer cells through GPCRs. Deregulation of the LPA signaling axis has been linked to different diseases, such as liver disease, fibrosis, pruritus, multiple sclerosis, inflammation, and cancer. A specific ENPP2 inhibitor against idiopathic pulmonary fibrosis showed promising results in the clinical trial, and the inhibition of ENPP2 also can stimulate T-cell infiltration into tumors and enhance the efficacy of immunotherapy for liver disease and pancreatic cancer.
Family:
Phosphatase
Class:
Protein (enzyme)
Protein Name:
ENPP2
Uniprot Number:
Q13822
Protein Aliases:
Autotaxin; Extracellular lysophospholipase D (LysoPLD)
Gene Name:
ENPP2
Gene ID:
5168
Gene Aliases:
ATX; PD-IALPHA
Accession Number:
NM_001040092
Organism:
Human
Construct Details:
Fragment, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Platform:
Plate reader
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant protein ENPP2 expressed in mouse myeloma cells is used. Test compound and/or vehicle is preincubated with 0.136 µg/ml enzyme for 15 minutes at 37°C in modified Tris-HCl buffer pH 8.0. The reaction is initiated by addition of 0.5 µM FS-3 for 30 minutes. Determination of the amount of divided fluorescence parts formed is read spectrofluorimetrically at 485 nm/520 nm. Compounds are screened at 10 µM.
Substrate:
0.5 µM FS-3
Incubation:
30 min at 37°C
Control Inhibitor:
ONO-8430506
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