Activity-based PKCa kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
PKCa
Enzyme
Human PKCa
HGNC
PRKCA
Synonym
PRKACA, PKc-alpha
Substrates
Peptide substrate [ERMRPRKRQGSVRRRV], 20 µM, and Lipid activatorATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 0.4 |
| Ro 31-8220 | 0.3 |
| GW 5074 | 4,300 |
| H-89 | 2,700 |
| Rottlerin | >100,000 |
Scientific Information
P17252 (http://www.uniprot.org/uniprot/P17252)
Screening Location
Malvern, USA
Reference compound IC50 for PKCa
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