Biological Information

Background Information:

PTPRM (PTPRM, RPTPmu, RPTPU), a member of the protein tyrosine phosphatase (PTP) family, is thought to play an important role in cell-cell adhesion mediated processes. PTPs have high substrate specificity for phosphotyrosyl proteins, at the primary sequence level sharing little similarity with the protein serine phosphatases, protein threonine phosphatases, or the acid and alkaline phosphatases. The specific expression of PTPRM in arterial endothelial cells and cardiac myocytes suggests a possible role in the regulation of cardiovascular functions. PTPRM has been implicated in playing a tumour suppressor role in kidney, lung and breast cancers.

Family:

Phosphatase

Sub Family:

RTP

Class:

Protein Tyrosine

Protein Name:

PTPRM

Uniprot Number:

P28827

Gene Name:

PTPRM

Gene ID:

5797

Gene Aliases:

RPTPU|hR-PTPu

Accession Number:

NM_001105244

Organism:

Human

Construct Details:

Fragment (839-1100), 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 RPTPm expressed in E. coli is used. Test compound and/or vehicle is preincubated with 62 ng/ml enzyme‡ for 15 minutes at 37°C in modified Tris-HCl buffer pH 8.5. 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

0.05μM - IC50

PubChem ID

5353574

Name

Dephostatin

Measurement

23μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

6.4μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

0.99μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

Inhibition of PTPRM may facilitate growth and metastasis of numerous cancers.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP260