Biological Information

Background Information:

PTPN9 (protein tyrosine phosphatase, non-receptor type 9, MEG2) was originally cloned from human MEG-01 megakaryocyte and umbilical vein endothelial cell cDNA. The full-length enzyme has been reported to bind phospholipid with high affinity and that this binding is important for MEG2 activity on secretory vesicles. MEG2 is a polyphosphoinositide-activated tyrosine phosphatase that may be involved in signaling events regulating phagocytosis, essential antimicrobial function in the immune response, development of erythroid cells and insulin desensitization.

Family:

Phosphatase

Sub Family:

Non-Receptor

Class:

Protein Tyrosine

Protein Name:

PTPMEG2

Uniprot Number:

P43378

Gene Name:

PTPN9

Gene ID:

5780

Gene Aliases:

MEG2

Accession Number:

NM_002833

Organism:

Human

Construct Details:

Fragment (285-593), 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 protein phosphatase MEG2 expressed in E. coli is used. Test compound and/or vehicle is preincubated with 7.8 ng/ml enzyme‡ for 15 minutes at 37°C in modified Tris-HCl buffer pH 7.2. The reaction is initiated by addition of 100 μM DiFMUP for 60 minutes. Determination of the amount of DiFMU formed is read spectrofluorimetrically at 358 nm/450 nm. Compounds are screened at 10 µM.

Substrate:

100 µM DiFMUP

Incubation:

60 min at 37°C

Control Inhibitor:

(NH₄)₆Mo₇O₂₄

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

61671

Name

Trisodium vanadate

Measurement

0.11μM - IC50

PubChem ID

5353574

Name

Dephostatin

Measurement

41μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

3.5μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

0.39μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

Inhibition of MEG2 may facilitate microbial infections, reduce development of erythroid cells (especially those in polycythemia vera patients), and restore insulin sensitivity in type 2 diabetes.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP260