A GSK3β inhibitor (Ki = 4.9 nM) that crosses the blood brain barrier and inhibits tau phosphorylation (IC50 = 76 nM in vitro); stabilizes β-catenin and increases bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily

AZD 2858 – 1 mg

Brand:
Cayman
CAS:
486424-20-8
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} It can also phosphorylate proteins that are relevant to osteogenesis and Alzheimer’s disease, the latter for which it has earned the moniker, tau phosphorylating kinase.{25567,25565,25566} AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM.{27205} It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM.{27205} AZD 2858 has also been shown to increase bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily.{27203} Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.{27204}  

 

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Description

A GSK3β inhibitor (Ki = 4.9 nM) that crosses the blood brain barrier and inhibits tau phosphorylation (IC50 = 76 nM in vitro); stabilizes β-catenin and increases bone mass (via Wnt activation) in rats after a two-week treatment with a maximum effective oral dose of 20 mg/kg once daily

Formal name: 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide

Synonyms: 

Molecular weight: 453.5

CAS: 486424-20-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Stem Cell Research|Differentiation||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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