Biological Information

Background Information:

PTPN12 (Tyrosine-protein phosphatase non-receptor type 12, PTP-PESTPTPG1) is a ubiquitously expressed cytosolic protein tyrosine phosphatase. PTP-PEST contains the typical tyrosine phosphatase catalytic domain flanked by proline-rich regions that are shown to interact with several signaling proteins including Grb2, paxillin, p130CAS and other adhesion molecules. PTP-PEST is involved in negatively regulating specific aspects of T cell development.

Family:

Phosphatase

Sub Family:

Non-Receptor

Class:

Protein Tyrosine

Protein Name:

PTP-PEST

Uniprot Number:

Q05209

Gene Name:

PTPN12

Gene ID:

5782

Gene Aliases:

PTPG1|PTP-PEST

Accession Number:

NM_002835

Organism:

Human

Construct Details:

Fragment (2-300), 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 PEST expressed in E. coli is used. Test compound and/or vehicle is preincubated with 2.8 ng/ml enzyme‡ for 15 minutes at 37°C in modified HEPES 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

0.24μM - IC50

PubChem ID

5353574

Name

Dephostatin

Measurement

66μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

1.6μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

0.25μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

Inhibition of PTP-PEST may reduce cell migration and spreading of fibroblasts resulting in impaired wound healing.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei