PTEN Human Phosphatase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
PTEN (phosphatase and tensin homologue deleted on chromosome ten; MMAC1, TEP1) is a dual-specificity phosphatase (with both protein and lipid phosphatase activity) first identified as a tumor suppressor gene. PTEN negatively regulates intracellular levels of phosphatidylinositol-3,4,5-triphosphate in cells and functions as a tumor suppressor by negatively regulating AKT/PKB signaling pathway. Its role in tumor suppression is confirmed by frequent endometrial abnormalities which develop in PTEN-deficient mice and high incidence of breast, thyroid, and endometrial cancers in humans with constitutive mutation of one PTEN allele, Cowden’s syndrome.
Family:
Phosphatase
Sub Family:
Dual Specificity
Class:
Lipid
Protein Name:
PTEN
Uniprot Number:
P60484
Protein Aliases:
mutated in multiple advanced cancers 1
Gene Name:
PTEN
Gene ID:
5728
Gene Aliases:
MMAC1|TEP1|PTEN1
Accession Number:
NM_000314
Organism:
Human
Construct Details:
Full Length, 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 phosphatase PTEN expressed in E. coli is used. Test compound and/or vehicle is preincubated with 2 μg/ml enzyme‡ for 15 minutes at 37⁰C 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
Clinical Relevance
Adverse / Beneficial Action:
Inhibitorsof PTEN maypromote tumor proliferation and metastasisby inhibiting the enzyme's tumor-supressive activity.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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