Biological Information
Background Information:
ERK1 (extracellular signal-regulated protein kinase) is one of the isoforms of MAP kinase. This 42 kD serine/threonine kinase is activated by dual phosphorylation on tyrosine and threonine residues. Phosphorylation of both residues by the upstream activator MEK is essential not only for ERK1 activation but also for translocation of the ERK1 to the nucleus. Following this activation, ERK1 phosphorylates a large number of regulatory proteins and this directly controls key cellular processes such as transcription, translation and cytoskeletal rearrangement. An inhibitor assay may be of benefit for the treatment of cancer, diabetes, neurodegenerative disorders or asthma.
Family:
Kinase
Sub Family:
CMGC
Class:
Protein Ser/Thr
Protein Name:
ERK1
Uniprot Number:
P27361
Protein Aliases:
MAPK 3|ERT2|Extracellular signal-regulated kinase 1|ERK-1|Insulin-stimulated MAP2 kinase|MAP kinase isoform p44|p44-MAPK|Microtubule-associated protein 2 kinase|p44-ERK1
Gene Name:
MAPK3
Gene ID:
5595
Gene Aliases:
ERK1|p44mapk|p44erk1|PRKM3
Accession Number:
NM_001109891
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant protein kinase ERK1 expressed in E. coli is used. Test compound and/or vehicle is incubated with 200 ng/ml enzyme‡ in MOPS buffer pH 7.2 for 30 minutes at 37°C. The reaction is initiated by addition of 50 μg/ml myelin basic protein (MBP), 10 μM ATP and [γ32P]ATP for another 30 minute incubation period and terminated by cooling on ice. An aliquot is then removed and counted to determine the amount of [32P]MBP (myelin basic protein) formed. Compounds are screened at 10 μM.
Substrate:
50 µg/ml Myelin basic protein (MBP)
ATP Concentration:
10 uM
Incubation:
30 min at 37°C
Control Inhibitor:
Staurosporine
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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