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Data

Product overview

  • Name
    SB 216763
  • Short description
    Potent, selective cell permeable GSK-3 inhibitor
  • Biological description

    Potent, selective, cell permeable and ATP competitive GSK-3 inhibitor which is equally effective at GSK-3α as GSK-3β (IC50 = 34 nM for GSK-3α). Displays little activity at 24 other serine/threonine and tyrosine protein kinases.

    SB 216763 is active in vivo.


    The compound stimulates glycogen synthesis (EC50 = 3.6 µM), acts as a neuroprotectant and prevents neuronal cell death. It also shows anti-inflammatory and cardioprotective actions. 


    It is also widely used in stem cell research, for example:


    Maintenance

    • Maintains mESCs (mouse embryonic stem cells) in a pluripotent state in the absence of LIF when cultured with MEFs
    • Restores insulin-dependent differentiation of C2ind myoblasts

    Differentiation

    • Promotes the conversion of human umbilical cord mesenchymal stem cells into neural precursors
    • Enhances chondrogenic differentiation of hWJ-MSCs
    • Increases neurogenesis of human neural progenitor cell differentiation
    • Promotes neural differentiation of CD117-positive hAFS cells towards neural progenitor cells

    Proliferation

    • Promotes the proliferation of retinal stem cells
  • Alternative names
    SB-216763
  • Biological action
    Inhibitor
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
  • Molecular Weight
    371.22
  • Molecular Formula
    C19H12Cl2N2O2
  • CAS Number
    280744-09-4
  • PubChem identifier
    176158
  • SMILES
    CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl
  • Source
    Synthetic
  • InChi
    InChI=1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
  • InChiKey
    JCSGFHVFHSKIJH-UHFFFAOYSA-N
  • MDL number
    MFCD09753369
  • Appearance
    Orange solid

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in DMSO (75mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for SB 216763

  • Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.

    Coghlan MP et al (2000) Chem Biol 7(10) : 793-803.
    PubMedID: 11033082
  • 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.

    Gurrieri C et al (2010) J Pharmacol Exp Ther 332(3) : 785-94.
    PubMedID: 19959748
  • Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.

    Cross DA et al (2001) J Neurochem 77(1) : 94-102.
    PubMedID: 11279265
  • Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.

    Kirby et al (2012) PLoS One 6 : e39329
    PubMedID: 22745733
  • Stemistry: the control of stem cells in situ using chemistry.

    Davies et al (2015) J Med Chem 58(7) : 2863-94
    PubMedID: 25590360
  • Activation of canonical Wnt pathway promotes proliferation of retinal stem cells derived from adult mouse ciliary margin.

    Inoue et al (2006) Stem Cells 24(1) : 95-104
    PubMedID: 16223856
  • Glycogen synthase kinase 3 (GSK3)-inhibitor SB216763 promotes the conversion of human umbilical cord mesenchymal stem cells into neural precursors in adherent culture.

    Gao et al (2017) Hum Cell 30(1) : 11-22
    PubMedID: 27604750
  • Insulin and wnt1 pathways cooperate to induce reserve cell activation in differentiation and myotube hypertrophy.

    Rochat et al (2004) Mol Biol Cell 15(10) : 4544-55
    PubMedID: 15282335
  • Small molecule GSK-3 inhibitors increase neurogenesis of human neural progenitor cells.

    Lange et al (2011) Neurosci Lett. 488(1) : 36-40
    PubMedID: 21056624
  • Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion.

    Gross et al (2008) Am J Physiol Heart Circ Physiol 294(3) : 1495-500
    PubMedID: 18223186
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