OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
ERKs (extracellular signal-regulated kinase) are activated by the MEK (mitogen-activated protein kinase, or ERK kinase). MEKs are activated by members of the Raf family. The signaling pathway comprising Raf and ERK (extracellular signal-regulated kinase) lies downstream of the small guanine nucleotide binding protein Ras and mediates several apparently conflicting cellular responses, such as proliferation, apoptosis, growth arrest, differentiation, and senescence, depending on the duration and strength of the external stimulus and on cell type. An inhibitor assay may be of benefit for the treatment of cancer, diabetes, neurodegenerative disorders or asthma.
Family:
Kinase
Sub Family:
STE
Class:
Protein Ser/Thr
Protein Name:
MEK1
Uniprot Number:
Q02750
Protein Aliases:
MAPKK 1|MKK1|ERK activator kinase 1|MAPK/ERK kinase 1|MEK 1
Gene Name:
MAP2K1
Gene ID:
5604
Gene Aliases:
MEK1|MAPKK1|PRKMK1
Organism:
Human
Construct Details:
Full length recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
MEK1 (h) is incubated with 50 mM Tris pH 7.5, 0.2 mM EGTA, 0.1% 6-mercaptoethanol, 0.01% Brij-35, 1 µM unactive MAPK2 (m), 10 mM MgAcetate and cold ATP (concentration as required). The reaction is initiated by the addition of the Mg/ATP. After incubation for 40 minutes at room temperature, 5 uL of this incubation mix is used to initiate a MAPK2 (m) assay.
Substrate:
1 uM unactive MAPK2
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= ND )
Incubation:
40 min at Room temperature
Control Inhibitor:
Acid Blank
Test Sample Requirements:
Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
MEK1 Human STE Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-429KP10
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