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:

Endothelial tyrosine kinase|Tunica interna endothelial cell kinase|Tyrosine kinase with Ig and EGF homology domains-2|Tyrosine-protein kinase receptor TEK|Tyrosine-protein kinase receptor TIE-2|hTIE2|p140 TEK|CD antigen CD202b

Gene Name:

TEK

Gene ID:

7010

Gene Aliases:

TIE2|TIE-2|VMCM1|CD202b

Accession Number:

NM_000459

Organism:

Human

Construct Details:

Fragment (771-end), Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant protein kinase TIE2 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.13 U/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.4. The reaction is initiated by addition of 0.2 mg/ml poly(Glu:Tyr), 10 µM ATP containing 0.25 µCi [γ32P]ATP for 30 minutes and terminated by further addition of 3% H3PO4. An aliquot is counted to determine the radioactivity of [32P]Poly(Glu:Tyr). Compounds are screened at 10 µM.

Substrate:

200 µg/ml Poly(Glu:Tyr)

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

Staurosporine

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

5328760

Name

Tyrphostin AG 538

Measurement

0.18μM - IC50

PubChem ID

122130844

Name

Staurosporine

Measurement

0.037μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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Item: PP90