GSK3alpha Human CMGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Glycogen synthase kinase 3 (GSK3) is a protein kinase that was originally identified as a regulator of glycogen synthase, a key enzyme in glycogen metabolism. There exists two isoforms of GSK3, GSK3A and GSK3B, and they are strictly regulated via phosphorylation. GSK3 has been shown to phosphorylate a number of different cellular proteins, including p53, c-Myc, c-Jun, heat shock factor-1 (HSF-1), and cyclin D1. GSK3A also has been inhibited by activation of the canonical Wnt pathway, resulting in increased catenin that drives human mesenchymal stem cells to osteoblasts.
Family:
Kinase
Sub Family:
CMGC
Class:
Protein Ser/Thr
Protein Name:
GSK3alpha
Uniprot Number:
P49840
Protein Aliases:
Serine/threonine-protein kinase GSK3A
Gene Name:
GSK3A
Gene ID:
2931
Accession Number:
NM_019884
Organism:
Human
Construct Details:
Fragment (2-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 GSK3A expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.16 U/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 5 µM phospho-glycogen synthase peptide-2, 10 µM ATP and 0.25 µCi [γ32P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Phospho-glycogen synthase peptide-2 formed. Compounds are screened at 10 µM.
Substrate:
5 µM Phospho-glycogen synthase peptide-2
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:
Metabolic Diseases
Adverse / Beneficial Action:
Inhibitors may have therapeutic potential for the treatment of diabetes, Alzheimer's disease, osteoblast differentiation, stroke and bipolar disorder.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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