Tie2 (Y897S) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-764KP10

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

The TIE family of receptor tyrosine kinases comprises two members, TIE1 and TIE2 (Angiopoietin 1 receptor, Tyrosine-protein kinase receptor TIE-2, Tyrosine-protein kinase receptor TEK, P140 TEK, Tunica interna endothelial cell kinase, CD202b antigen, EC 2.7.1.112 ). These receptors are expressed predominantly in endothelial cells and are essential for vessel formation where they are required for the later stages of angiogenesis and vessel maintenance. TIE2 has roles in control of microvessel sprouting, integrity, and maturation. Angiopoietin-1 (Ang1) and angiopoietin-2 (Ang2) have been identified as ligands of TIE2 receptor, which may regulate endothelial cell proliferation, differentiation and guide the proper patterning of endothelial cells during blood vessel formation. Inhibitors of TIE2 may inhibit vascular healing and tumor angiogenesis.

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

TIE2

Uniprot Number:

Q02763

Protein Aliases:

Gene Name:

TEK

Gene ID:

7010

Gene Aliases:

TIE2|TIE-2|VMCM1|CD202b

Accession Number:

NM_000459

Organism:

Human

Construct Details:

771-end; Q939H; Q940H; Y897S recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Tie2 (Y897S) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2, 400 µM EFPIYDFLPAKKK, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.

Substrate:

400 uM EFPIYDFLPAKKK

Tracer:

33P

ATP Concentration:

[ATP]= 10µM (Km= 41µM )

Incubation:

40 min at Room temperature

Control Inhibitor:

Staurosporine

Test Sample Requirements:

Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.

Minimum Order Quantity:

Turnaround Time

Standard:

6 Business Days

Service Scheduling Note:

Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

26.57nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault