Activity-based ERBB2/HER2 kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ERBB2/HER2
Enzyme
Human ERBB2/HER2
HGNC
ERBB2
Synonym
NEU, NGL, HER2, TKR1
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.2 mg/ml
ATP 10 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 60 |
| PP2 | 230 |
| AG1478 | 6.5 |
| EGFR/Erb Inhibitor | 0.1 |
| D-64406 | >100,000 |
Scientific Information
P04626 (http://www.uniprot.org/uniprot/P04626)
Screening Location
Malvern, USA
Reference compound IC50 for ERBB2/HER2
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