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. SGK1 (SGK) is predominately expressed in kidney, liver and pancreas. The catalytic domain of serum/glucocorticoid regulated protein kinase is most similar to PKB and activated via phosphorlation mechanism when cells are stimulated with insulin, IGF1 or serum, or exposed to oxidative stress.
Family:
Kinase
Sub Family:
AGC
Class:
Protein Ser/Thr
Protein Name:
SGK1
Uniprot Number:
O00141
Protein Aliases:
Serum/glucocorticoid-regulated kinase 1
Gene Name:
SGK1
Gene ID:
6446
Accession Number:
NM_005627
Organism:
Human
Construct Details:
Fragment (60-end), 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 SGK1 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.3 U/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 10 µM crosstide KK, 10 µM ATP and 0.25 µCi [γ32P]ATP for another 30 minutes incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Crosstide KK formed. Compounds are screened at 10 µM.
Substrate:
10 µM Crosstide KK
ATP Concentration:
10 uM
Incubation:
30 min at 37°C
Control Inhibitor:
Staurosporine
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:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
SGK1 inhibitors may have therapeutic potential in hypertension, diabetes and cancer treatment.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei