OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
p21-activated kinases (PAK) are serine/threonine kinases, which consist of the three highly homologous members PAK1 to -3, regulated by the GTPases Rac1 and Cdc42. PAKs are numerous and include morphogenetic regulation, modulation of signaling cascades leading to transcriptional regulation, and regulation of apoptotic pathways. PAK2 (PAK65) can monophosphorylate the myosin II regulatory light chain and induce retraction of permeabilized endothelial cells. PAK2 also can be activated by caspase-cleavage in addition to p21-binding. PAK2 inhibitors may have therapeutic potential in cancer treatment.
Family:
Kinase
Sub Family:
STE
Class:
Protein Ser/Thr
Protein Name:
PAK2
Uniprot Number:
Q13177
Protein Aliases:
S6/H4 kinase
Gene Name:
PAK2
Gene ID:
5062
Gene Aliases:
PAK65|PAKgamma
Accession Number:
U24153
Organism:
Human
Construct Details:
3-end; L150F; P225T; A339 deleted; V383I recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
PAK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 µM KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK, 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 µM KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 89µM )
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:
PAK2 inhibitors may have therapeutic potential in cancer treatment.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
PAK2 Human STE Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-481KP
Questions? Contact Us
You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.
