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AZD2858
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C21H23N7O3S
- MW: 453.52
Description
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.
More Information
| Parent CAS No. | 486424-20-8 |
|---|---|
| Chemical Name | 3-Amino-6-(4-(4-methylpiperazin-1-ylsulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide |
| SMILES | C1N=C(N)C(C(=O)NC2=CC=CN=C2)=NC=1C1=CC=C(S(N2CCN(C)CC2)(=O)=O)C=C1 |
| MFCD | MFCD26397072 |
| InChi | InChI=1S/C21H23N7O3S/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) |
| InChiKey | FHCSBLWRGCOVPT-UHFFFAOYSA-N |
| CID | 10138980 |
| Short Description | GSK-3β inhibitor |
References
- 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.
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