Biological Information

Background Information:

PTP1B is a major intracellular protein tyrosine phosphatase first isolated from human placenta. It consists of a single catalytic domain and a hydrophobic carboxyl terminus responsible for localizing the enzyme to the endoplasmic reticulum. PTP1B is involved in regulating tyrosine kinases by controlling their phosphorylation status. Overexpression of this enzyme has been linked to several oncogenic diseases. Studies conducted on frozen sections from ovarian and breast cancer patients indicate increased expression of PTP1B along with protein tyrosine kinases. Inhibitors of PTP1B may be of potential therapeutic use for the treatment of breast and ovarian cancer.

Family:

Phosphatase

Sub Family:

Non-Receptor

Class:

Protein Tyrosine

Protein Name:

PTP1B

Uniprot Number:

P18031

Gene Name:

PTPN1

Gene ID:

5770

Accession Number:

NM_001278618

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 PTP1B expressed in E. coli is used. Test compound and/or vehicle is preincubated with 170 µU/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

0.016μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

0.25μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

0.029μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP260