Biological Information
Background Information:
The serum/glucocorticoid regulated kinases (SGK1,2,3) are serine/threonine kinases that belong to the AGC (protein kinase A; protein kinase G and protein kinase C) subfamily that includes cAMP and cGMP dependent kinases, PKB and PKC. SGK predominately expressed in kidney, liver and pancreas. The catalytic domain of serum/glucocorticoid regulated protein kinase (SGK) is most similar to PKB and activated via phosphorlation mechanism when cells are stimulated with insulin, IGF1 or serum, or exposed to oxidative stress. SGK2 inhibitors may have therapeutic potential in renal hypertension.
Family:
Kinase
Sub Family:
AGC
Class:
Protein Ser/Thr
Protein Name:
SGK2
Uniprot Number:
Q9HBY8
Protein Aliases:
Serum/glucocorticoid-regulated kinase 2
Gene Name:
SGK2
Gene ID:
10110
Accession Number:
NM_016276
Organism:
Human
Construct Details:
54-end; S416D recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
SGK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 µM GRPRTSSFAEGKK, 10 mM MgAcetate and [g- 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 GRPRTSSFAEGKK
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 18.87µM )
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:
Renal
Adverse / Beneficial Action:
SGK2 inhibitors may have therapeutic potential in treatment of renal hypertension.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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