ERK2 (MAPK1) Human CMGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
MAPK1 (mitogen-activated protein kinase 1, ERK2 or extracellular signal –regulated protein kinase) is one of the isoforms of MAP kinase. This serine/threonine kinase is activated by dual phosphorylation on tyrosine and threonine residues (Tyr-185 and Thr-183). Phosphorylation of both residues by the upstream activator MEK (mitogen-activated protein kinase kinase, MAP2K) is essential not only for ERK2 activation, but also for translocation of the ERK2 to the nucleus. Following this activation, ERK2 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:
ERK2
Uniprot Number:
P28482
Protein Aliases:
MAPK 1|Extracellular signal-regulated kinase 2|ERK-2|MAP kinase isoform p42|p42-MAPK|Mitogen-activated protein kinase 2|MAP kinase 2|MAPK 2
Gene Name:
MAPK1
Gene ID:
5594
Gene Aliases:
ERK|ERK2|p41mapk|MAPK2|PRKM1|PRKM2
Accession Number:
NM_138957
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 ERK2 expressed in E. coli is used. Test compound and/or vehicle is preincubated with 1 U/ml enzyme‡ in MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 50 μg/ml myelin basic protein (MBP), 10 μM ATP and 0.25 μCi [γ32P]ATP for another 30 minute incubation period and terminated by cooling on ice. An aliquot is removed and counted to determine the amount of [32P]MBP 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:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
DrugMatrixScreen LeadHunter Panel - TW
Item: PP89
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