Activity-based PKCtheta kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
PKCtheta
Enzyme
Human PKCtheta
HGNC
PRKCQ
Synonym
PRKCT, nPKC-theta
Substrates
Peptide substrate [ERMRPRKRQGSVRRRV], Lipid activator, 20 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 0.2 |
| Ro 31-8220 | <0.1 |
| GW5074 | 6,300 |
| H-89 | 600 |
| Rottlerin | >100,000 |
Scientific Information
Q04759 (http://www.uniprot.org/uniprot/Q04759)
Screening Location
Malvern, USA
Reference compound IC50 for PKCtheta
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