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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: GSK3 (Glycogen synthase kinase) is a monomeric serine/threonine kinase, from the CMGC (cyclin-dependent kinase, mitogen-activated protein kinases, GSK and CDC-like kinase) group and has two isozymes: GSK3α and GSK3β. GSK3α, with only one mRNA, has a similar structure to the other isozyme, which has two isoforms, but has an N-terminal domain that is longer and enriched in glycine. GSK3α is found mostly in the cytosol, while GSK3β can also be found in the nucleus and mitochondria, endosomes, and lysosomes. It is involved in glucose metabolism, mitochondrial activity, cell proliferation and apoptosis, amongst others, acting through the more than 40 known targets and 500 proposed ones. It is normally present as an active protein in resting cells, but its activity can be modulated by post-translational modifications. For instance, phosphorylation of Try279 in GSK3α and Tyr216 in GSK3β can potentiate its activity by 5-fold. It is an important regulator enzyme in many diseases including cancer, immune disorders, metabolic disorders such as diabetes and obesity, inflammatory diseases such as RA (rheumatoid arthritis) and neurological disorders like Alzheimer's disease. Active GSK3 regulates several pro-inflammatory cytokines, chemokines, and molecules such as prostaglandin E2. The use of inhibitors is thus an attractive strategy for the treatment of inflammatory disorders.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ GSK3α Kinase Assay Kit is designed to measure GSK3α (Glycogen Synthase Kinase 3 Alpha) serine/threonine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified GSK3α, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P49840
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: McCubrey J.A., et al., 2014 Oncotarget 5(10): 2881-2911.
Hoffmeister L., et al., 2020 Cells 9(4):820.
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