SAPK2A (p38alpha) Human CMGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

Item: 176610

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Mitogen-activated protein (MAP) kinases are proline-directed protein kinases that mediate the effects of numerous extracellular stimuli on a wide array of biological processes, such as cellular proliferation, differentiation, and death. Three groups of mammalian MAP kinases have been studied in detail: the extracellular signal-regulated kinases (ERK), the c-Jun NH2-terminal kinases (JNK), and the p38 MAP kinases. The p38 MAP kinase group, which includes the isoforms p38a, p38b, p38g and p38d, activates the transcription factors CREB, ATF1, ATF2, CHOP, and MEF-2C. The p38 MAP kinase also activates other protein kinases, such as Mapkap-2, Mapkap-3, and Mnk1/2.

Family:

Kinase

Sub Family:

CMGC

Class:

Protein Ser/Thr

Protein Name:

p38alpha (SAPK2A)

Uniprot Number:

Q16539

Protein Aliases:

p38 MAP kinase

Gene Name:

MAPK14

Gene ID:

1432

Gene Aliases:

Accession Number:

NM_001315

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 P38α expressed in E. coli is used. Test compound and/or vehicle is preincubated with 74.5 mU/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 50 μg/ml MBP, 10 μM ATP and 0.25 μCi [γ32P]ATP and incubated for 30 minites. The reaction is terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [γ32P]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:

SB 202190

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5353940

Name

SB 202190

Measurement

0.01μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

nhibition of MAPK14 may reduce inflammation, cell proliferation, cell differentiation and apoptosis.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei