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
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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