Activity-based DYRK1/DYRK1A kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
DYRK1/DYRK1A
Enzyme
Human DYRK1/DYRK1A
HGNC
DYRK1A
Synonym
DYRK, DYRK1, HP86, MNB, MNBH
Substrates
Peptide substrate, [RRRFRPASPLRGPPK], 20 µM
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 | 3.8 |
| Ro 31-8220 | 23 |
| GW5074 | 420 |
| H-89 | >20,000 |
| Rottlerin | >20,000 |
Scientific Information
Q13627 (http://www.uniprot.org/uniprot/Q13627)
Screening Location
Malvern, USA
Reference compound IC50 for DYRK1/DYRK1A
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