Biological Information

Background Information:

PTPRF, protein tyrosine phosphatase, receptor type, F (LAR or leukocyte common antigen-related molecule;) is a phospho tyrosine-specific protein phosphatase. Human LAR is expressed in various cell lineages such as epithelial cells, smooth muscle cells, and cardiac myocytes, but not in the spleen, brain, or neurons. Physiological function for LAR in cellular signalling by tyrosine dephosphorylation is responsive to cell-cell or cell-matrix interactions. An LAR inhibitor may be useful in the treatment of insulin resistance.

Family:

Phosphatase

Sub Family:

RTP

Class:

Protein Tyrosine

Protein Name:

LAR

Uniprot Number:

P10586

Gene Name:

PTPRF

Gene ID:

5792

Accession Number:

NM_001329137

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 protein phosphatase LAR expressed in E. coli is used. Test compound and/or vehicle is preincubated with 0.48 ng/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.2. The reaction is initiated by addition of 10 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:

10 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

0.043μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

0.29μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

0.11μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

An LAR inhibitor may be useful in the treatment of insulin resistance.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei