For research use only. Not for therapeutic Use.
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 free base AZD2858 is available as Axon 3771.
KEYWORDS: AZD2858 hydrochloride | GSK3â inhibitor | GSK3 | GSK-3 | AZD-2858 | AZD-2858 | Wnt | osteoporosis | Alzheimer’s | AD | amyloid | tau | CDK2 | glycogen | synthase
| Catalog Number | I047600 |
| CAS Number | 2108876-05-5 |
| Molecular Formula | C21H23N7O3S.HCl |
| Purity | ≥95% |
| IUPAC Name | 3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-N-pyridin-3-ylpyrazine-2-carboxamide;hydrochloride |
| InChI | InChI=1S/C21H23N7O3S.ClH/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16;/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29);1H |
| SMILES | CN1CCN(CC1)S(=O)(=O)C2=CC=C(C=C2)C3=CN=C(C(=N3)C(=O)NC4=CN=CC=C4)N.Cl |
| Reference | S. Berg et al. Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer’s disease: design, synthesis, and characterization of pyrazines. J. Med. Chem. 2012, 55, 9107-9119.
R. Marsell et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012, 50, 619-627. |
