产品描述:
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}