Activity-based TIE mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
TIE2
Enzyme
Human TIE2
HGNC
TEK
Synonym
Angiopoietin-1 receptor [Precursor], Tyrosine-protein kinase receptor TIE-2, hTIE2, Tyrosine-protein kinase receptor TEK, p140 TEK, Tunica interna endothelial cell kinase
Scientific Information
Q02763 (http://www.uniprot.org/uniprot/Q02763)
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
| Mutant | Staurosporine | PP2 | AG1478 | PDGFR I-III | EGFR/ErbB Inhibitor | D-64406 |
|---|---|---|---|---|---|---|
| WT | 11.2 | 4,400 | 6,700 | n.a. | n.a. | 5,300 |
| A1124V | 37 | 5,400 | 13,000 | 35,000 | n.a. | 21,000 |
| P883A | 39 | 4,200 | 6,600 | 24,000 | n.a. | 30,000 |
| R849W | 15 | 6,300 | 15,000 | >100,000 | n.a. | >100,000 |
| Y1108F | 16 | 12,000 | 17,000 | >100,000 | n.a. | >100,000 |
| Y897C | 120 | 19,000 | 26,000 | >100,000 | n.a. | >100,000 |
| Y897S | 190 | >100,000 | >100,000 | >100,000 | n.a. | >100,000 |
| Y897H/R915C | 430 | >100,000 | >100,000 | n.a. | >100,000 | >100,000 |
| Y897H | 55 | 26,000 | >100,000 | n.a. | >100,000 | >100,000 |
| R915C | 82 | 40,000 | >100,000 | n.a. | >100,000 | >100,000 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays.
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