Overview

  • Product name

    AZD2858, GSK-3 inhibitor
  • Description

    Selective GSK-3 inhibitor
  • Biological description

    Selective GSK-3 inhibitor (IC50 = 68 nM) of tau phosphorylation at the S396 site, activating Wnt signaling pathway. Greater than 70-fold selective against a panel of other kinases, receptors and enzymes. Stabilizes β-catenin in human and rat mesenchymal stem cells, stimulates hADSC commitment towards osteoblasts and osteogenic mineralisation in vitro. Promotes in vivo increase of bone mass in rats.

  • Purity

    > 99%
  • CAS Number

    486424-20-8
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    3-Amino-6-[4-[(1-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide

  • Molecular weight

    453.52
  • Molecular formula

    C21H23N7O3S
  • PubChem identifier

    10138980
  • Storage instructions

    Shipped at 4°C. Store at -20°C long term.
  • Solubility overview

    Soluble in DMSO to 15 mM and in 30% PEG400 + 0.5% Tween80 + 5% propylene glycol to 66 mM

  • SMILES

    CN1CCN(CC1)S(=O)(=O)C2=CC=C(C=C2)C3=CN=C(C(=N3)C(=O)NC4=CN=CC=C4)N
  • Source

    Synthetic

References

This product has been referenced in:

  • Gilmour PS  et al. Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats. Toxicol Appl Pharmacol 272:399-407 (2013). Read more (PubMed: 23872097) »
  • Marsell R  et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone 50:619-27 (2012). Read more (PubMed: 22142634) »

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