Activity-based GRK2 kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
GRK2
Enzyme
Human GRK2
HGNC
GRK2
Synonym
Beta-adrenergic receptor kinase 1, ARBK1, ADRBK1, BARK, BARK1, Beta-ARK-1
Scientific Information
P25098 (http://www.uniprot.org/uniprot/P25098)
Assay Properties
Substrates
Casein, 20 µM
ATP, 10 µM
ATP, 10 µM
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 |
|---|---|
| Staurosporine | 449 nM |
| Ro 31-8220 | 18.7 µM |
| GW 5074 | 13.6 µM |
| H-89 | 15.6 µM |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Screening Assay Services.
Reference compound inhibition of GRK2
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