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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS