OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating its deactivation. This gene has been linked to both genetic and acquired hypertension. Several transcript variants encoding different isoforms have been found for this gene.
Family:
Kinase
Sub Family:
AGC
Class:
Protein Serine/Threonine
Protein Name:
GRK4
Uniprot Number:
P32298
Protein Aliases:
IT11, GPRK4, GRK4a, GPRK2L
Gene Name:
GRK4
Gene ID:
2868
Gene Aliases:
GPRK2L, GPRK4a, IT11, GRK4
Organism:
Human
Construct Details:
Full length
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
GRK4 is incubated with 8mM MOPS, 0.2mM EDTA, 1.25 mg/ml Casein, 10 mM Magnesium acetate and [?-33P-ATP] (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 120 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:
1.25 mg/ml casein
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 59.8µM )
Incubation:
120 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:
Hypertension, blood pressure
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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.
