OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Mitogen-activated protein kinase (MAPK)-activated protein kinase 3 (MAPKAPK3) mediates multiple p38 MAPK-dependent inflammatory responses. This kinase can be activated in response to cellular stress and proinflammatory cytokines through its phosphorylation by MAP kinases including MAPK1/ERK, MAPK14/p38-alpha, and MAPK11/p38-beta. p38 MAP kinase, activated through MKK3, is required for the production of inflammatory cytokines by both antigen-presenting cells and CD4+ T cells.
Family:
Kinase
Sub Family:
CAMK
Class:
Protein Ser/Thr
Protein Name:
MAPKAPK3
Uniprot Number:
Q16644
Protein Aliases:
MAP kinase-activated protein kinase 3|MAPK-activated protein kinase 3; MAPKAP kinase 3; MAPKAP-K3; MAPKAPK-3; MK-3|Chromosome 3p kinase (3pK)
Gene Name:
MAPKAPK3
Gene ID:
7867
Gene Aliases:
3pK|MAPKAP3|3PK
Accession Number:
NM_004635
Organism:
Human
Construct Details:
2-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
MAPKAP-K3 (h) is incubated with 50 mM Na-b-glycerophosphate pH 7.5, 0.1 mM EGTA, 30 µM KKLNRTLSVA, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.
Substrate:
30 uM KKLNRTLSVA
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 102µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Staurosporine
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
Adverse / Beneficial Action:
MAPKAPK3 inhibition may reduce cell differentiation, proliferation and inflammation as well as cardiac reperfusion injury.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
MAPKAPK3 Human CAMK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-585KP
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