Biological Information
Background Information:
The protein tyrosine phosphatase, non-receptor type 11 (SHP-2) contains two tandem SH2 domain repeats at its N terminus and is expressed widely multiple growth factor receptor and cytokine pathways. Specifically, SHP-2 is thought to activate mitogen-activated protein kinase (MAPK) as the result of its direct action on PDGF and EGF growth factor receptors in response to ligand binding. Upregulation of SHP-2 activity is therefore believed to be a causative factor in vascular inflammation, tumor cell proliferation, and metastasis. More recently, SHP-2 deficiency has been shown to impair insulin sensitivity of glucose metabolism.
Family:
Phosphatase
Sub Family:
Non-Receptor
Class:
Protein Tyrosine
Protein Name:
SHP2
Uniprot Number:
Q06124
Gene Name:
PTPN11
Gene ID:
5781
Gene Aliases:
BPTP3|SH-PTP2|SHP-2|PTP2C|SHP2
Accession Number:
NM_001330437
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 PTPN11 (SHP-2) expressed in E. coli is used. Test compound and/or vehicle is preincubated with 45 ng/ml enzymeó for 15 minutes at 37°C in modified HEPES buffer pH 7.2. 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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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