Product Overview: 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
Glycogen synthase kinase 3β (GSK3β) was originally identified for its ability to constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis. 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. AZD 2858 is a pyrazine analog that inhibits GSK3β with a Ki value of 4.9 nM. It crosses the blood brain barrier and inhibits tau phosphorylation in vitro with an IC50 value of 76 nM. 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. Furthermore, by inhibiting GSK3β, AZD 2858 can stabilize β-catenin in rat mesenchymal stem cells (EC50 = 234 nM), spurring osteoblast differentiation.
Data:
Size: 1 mg
Shipping: wet ice
Stability: Store at -20 degrees; shelf life 730 days maximum after production
CAS Number: 486424-20-8
Molecular Formula: C21H23N7O3S
SMILES: NC1=NC=C(C2=CC=C(S(N3CCN(C)CC3)(=O)=O)C=C2)N=C1C(NC4=CC=CN=C4)=O
Molecular Weight: 453.5
Formulation: A crystalline solid
Purity: ≥98%
Custom Code: 2933599550
UNSPSC code: 12352100
Bertin Pharma
在过去的30年里,Bertin生物试剂在开发酶免疫分析试剂盒方面一直在开发一种独特的技术。
Over the past 30 years, Bertin Bioreagent has been developing a unique know-how in the development of enzyme immunoassay kits thanks to its outstanding scientific teams. This expertise is twofold: it enables the development of innovative and high quality products on biomarkers of interest and advises and accompanies our customers in their research.
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