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

PubChem ID

3035462

Name

Hymenialdisine

Measurement

1.3μM - IC50

PubChem ID

122130844

Name

Staurosporine

Measurement

0.015μM - IC50

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