Activity-based MEK1 kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
MEK1
Enzyme
Human MEK1
HGNC
MAP2K1
Synonym
MAPKK1, MKK1, PRKMK1
Substrates
ERK2 (K52R), 5 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 | 24 |
Ro 31-8220 | 16,800 |
GW 5074 | 3,600 |
H-89 | >100,000 |
Rottlerin | >100,000 |
Scientific Information
Q02750 (http://www.uniprot.org/uniprot/Q02750)
Screening Location
Malvern, USA
Reference compound IC50 for MEK1
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