Potent and highly selective Glycogen Synthase Kinase-3β (GSK-3β; Ki value 4.9 nM) inhibitor for Alzheimer’s disease with good BBB permeability in a bovine endothelial cell assay. AZD2858 inhibits GSK-3β-mediated tau phosphorylation (IC50 value 76 nM) in vitro, and shows a good overall selectivity versus a panel of 26 kinases and >100 fold selectivity over CDK2 (Ki value 540 nM). In rats, oral AZD2858 treatment caused a dose-dependent increase in trabecular bone mass by GSK-3 mediated inhibition of Wnt canonical signaling, making AZD2858 a possible therapeutic candidate for osteoporosis.

The water-soluble salt form, AZD2858 hydrochloride (Axon 2194), is also available. 

KEYWORDS: AZD2858 | Supplier | GSK-3β inhibitor | AZD-2858 | AZD 2858 | CAS [486424-20-8] | [2108876-05-5] | [486424-21-9] | Non Selective (Phosphorylation substrates) | GSK-3 | Inhibitor | Enzymes | Wnt | osteoporosis | Alzheimer's | AD | amyloid | tau | CDK2 | glycogen | synthase