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GSK-3 Inhibitors

Avistron Chemistry Services Products

GSK-3, originally identified in 1980, is one of the few signaling mediators that plays a central role in a diverse range of signaling pathways, including those activated by Wnts, hedgehog, growth factors, cytokines, and G protein-coupled ligands. It has been implicated in the mechanisms that regulate cellular proliferation, migration, inflammation and immune responses, glucose regulation, and apoptosis.

Although the original name suggests the enzyme is involved only in the process of glycogen metabolism, recent findings have revealed over 50 substrates that are phosphorylated by GSK-3, among them the microtubule-associated protein, tau, that is the predominant component of neurofibrillary tangles in Alzheimer’s disease. As lithium has been shown to potentially act through glycogen synthase kinase-3 (GSK3) inhibition, there is also a growing body of evidence suggesting that GSK-3 may be of interest in bipolar disorder (BD), animal models can be developed to probe the specific domains of this.

CHIR 99021 (AV02506) and SB627772 (AV00300) are highly potent inhibitors of GSK-3, and are amongst the compounds offered by Avistron. CHIR 99021 is a very potent and specific glycogen synthase kinase GSK-3 inhibitor which is often used in stem cell research.

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