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

PubChem ID

122130844

Name

Staurosporine

Measurement

0.57μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP89