Catalog Number: 1616
Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Biological Activity
Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 34.3 nM for GSK-3α). Equally effective at inhibiting human GSK-3α and GSK-3β. Exhibits minimal activity against 24 other protein kinases (IC50 >10 μM). Stimulates glycogen synthesis in liver cells, and induces β-catenin-dependent gene transcription. Neuroprotective; also reduces pulmonary inflammation and fibrosis in a mouse model. Shown to maintain mouse embryonic stem cells in a pluripotent state.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 75 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. 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 et al.
    J.Pharmacol.Exp.Ther., 2010;332:785
  2. Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival.
    Liang and Chuang
    J.Biol.Chem., 2006;282:3904
  3. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
    Coghlan et al.
    Chem.Biol., 2000;7:793
  4. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.
    Cross et al.
    J.Neurochem., 2001;77:94
  5. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.
    Kirby et al.
    PLoS One, 2012;7:e39329

The citations listed below are publications that use Tocris products. Selected citations for SB 216763 include:

Showing Results 1 - 10 of 50

  1. GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling.
    Authors: Stretton Et al.
    Biomed Res Int
  2. Glycogen synthase kinase-3 controls IL-10 expression in CD4(+) effector T-cell subsets through epigenetic modification of the IL-10 promoter.
    Authors: Hill Et al.
    Arch Med Sci
  3. Glycogen synthase kinase-3 (GSK3) inhibition induces prosurvival autophagic signals in human pancreatic cancer cells.
    Authors: Marchand Et al.
    Dev Cell
  4. Effects of kinesin-5 inhibition on dendritic architecture and microtubule organization.
    Authors: Kahn Et al.
    Mol Biol Cell
  5. Phosphorylation and SCF-mediated degradation regulate CREB-H transcription of metabolic targets.
    Authors: Barbosa Et al.
    Proc Natl Acad Sci U S A
  6. Morphine Reduces Myocardial Infarct Size via Heat Shock Protein 90 in Rodents.
    Authors: Small Et al.
    J Biol Chem
  7. Apelin-13 protects the heart against ischemia-reperfusion injury through the RISK-GSK-3β-mPTP pathway.
    Authors: Yang Et al.
    Mol Biol Cell
  8. Targeting β-arrestin2 in the treatment of L-DOPA-induced dyskinesia in Parkinson's disease.
    Authors: Urs Et al.
    Biochem J
  9. Extracellular α-synuclein leads to microtubule destabilization via GSK-3β-dependent Tau phosphorylation in PC12 cells.
    Authors: Gassowska Et al.
    PLoS One
  10. Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by insulin.
    Authors: Kuo Et al.
    J Lipid Res
  11. Phosphorylation of amyloid precursor protein at threonine 668 is essential for its copper-responsive trafficking in SH-SY5Y neuroblastoma cells.
    Authors: Acevedo Et al.
    Mol Endocrinol
  12. β-arrestin2/miR-155/GSK3β regulates transition of 5'-azacytizine-induced Sca-1-positive cells to cardiomyocytes.
    Authors: Zhao Et al.
    J Cell Biol
  13. Inhibiting glycogen synthase kinase-3 mitigates the hematopoietic acute radiation syndrome in mice.
    Authors: Lee Et al.
    Radiat Res
  14. Tristetraprolin mediates radiation-induced TNF-α production in lung macrophages.
    Authors: Ray Et al.
    PLoS One
  15. Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division.
    Authors: Robertson Et al.
    Mol Cancer
  16. Preventing p38 MAPK-mediated MafA degradation ameliorates β-cell dysfunction under oxidative stress.
    Authors: Khattabi and Sharma
    Hum Mol Genet
  17. N-cadherin specifies first asymmetry in developing neurons.
    Authors: Gärtner Et al.
    Mol Med
  18. Inhibition of GSK3 attenuates amphetamine-induced hyperactivity and sensitization in the mouse.
    Authors: Enman and Unterwald
    Neuro Oncol
  19. Death receptors DR6 and TROY regulate brain vascular development.
    Authors: Tam Et al.
    Eur J Immunol
  20. Glycogen synthase kinase 3β inhibitors protect hippocampal neurons from radiation-induced apoptosis by regulating MDM2-p53 pathway.
    Authors: Thotala Et al.
    Cell Death Differ
  21. Inhibition of GSK3 abolishes bacterial-induced periodontal bone loss in mice.
    Authors: Adamowicz Et al.
    Mol Cell
  22. Involvement of the glycogen synthase kinase-3 signaling pathway in TBI pathology and neurocognitive outcome.
    Authors: Dash Et al.
    PLoS One
  23. Inhibition of adipocytogenesis by canonical WNT signaling in human mesenchymal stem cells.
    Authors: Shen Et al.
    Exp Cell Res
  24. Glycogen synthase kinase-3 regulates cigarette smoke extract- and IL-1β-induced cytokine secretion by airway smooth muscle.
    Authors: Baarsma Et al.
    Am J Physiol Lung Cell Mol Physiol
  25. GSK3β inactivation induces apoptosis of leukemia cells by repressing the function of c-Myb.
    Authors: Zhou Et al.
    J Cell Mol Med
  26. The role of glycogen synthase kinase 3 in regulating IFN-β-mediated IL-10 production.
    Authors: Wang Et al.
    J Immunol
  27. Convergence of the mammalian target of rapamycin complex 1- and glycogen synthase kinase 3-β-signaling pathways regulates the innate inflammatory response.
    Authors: Wang Et al.
    J Immunol
  28. Glycogen synthase kinase 3β inhibition enhances repair of DNA double-strand breaks in irradiated hippocampal neurons.
    Authors: Yang Et al.
  29. Tumor-supportive and osteoclastogenic changes induced by breast cancer-derived factors are reversed by inhibition of {gamma}-secretase.
    Authors: Fong Et al.
    J Biol Chem
  30. Frizzled1 is a marker of inflammatory macrophages, and its ligand Wnt3a is involved in reprogramming Mycobacterium tuberculosis-infected macrophages.
    Authors: Neumann Et al.
  31. GSK3 inhibitors show benefits in an Alzheimer's disease (AD) model of neurodegeneration but adverse effects in control animals.
    Authors: Hu Et al.
    Neurobiol Dis
  32. p38 MAPK is a major regulator of MafA protein stability under oxidative stress.
    Authors: Kondo Et al.
    Mol Endocrinol
  33. c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells.
    Authors: Garcia Et al.
    J Immunol
  34. Toll-like receptor-mediated production of IL-1Ra is negatively regulated by GSK3 via the MAPK ERK1/2.
    Authors: Rehani Et al.
    J Immunol
  35. Phosphorylation of CLASP2 by GSK-3beta regulates its interaction with IQGAP1, EB1 and microtubules.
    Authors: Watanabe Et al.
    J Cell Sci
  36. Loss of PINK1 function affects development and results in neurodegeneration in zebrafish.
    Authors: Anichtchik Et al.
    J Neurosci
  37. Novel regulation of vascular endothelial growth factor-A (VEGF-A) by transforming growth factor (beta)1: requirement for Smads, (beta)-CATENIN, AND GSK3(beta).
    Authors: Clifford Et al.
    J Biol Chem
  38. Antigenic experience dictates functional role of glycogen synthase kinase-3 in human CD4+ T cell responses.
    Authors: Garcia Et al.
    J Immunol
  39. IFN-beta production by TLR4-stimulated innate immune cells is negatively regulated by GSK3-beta.
    Authors: Wang Et al.
    J Immunol
  40. A rational mechanism for combination treatment of Huntington's disease using lithium and rapamycin.
    Authors: Sarkar Et al.
    Hum Mol Genet
  41. Acidosis, oxygen, and interference with mitochondrial permeability transition pore formation in the early minutes of reperfusion are critical to postconditioning's success.
    Authors: Cohen Et al.
    Behav Brain Res
  42. Phosphatidylinositol 3-kinase regulation of gastrin-releasing peptide-induced cell cycle progression in neuroblastoma cells.
    Authors: Ishola Et al.
    Biol Open
  43. GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis.
    Authors: Lin Et al.
    J Cell Sci
  44. Polarity reveals intrinsic cell chirality.
    Authors: Xu Et al.
    Proc Natl Acad Sci U S A
  45. Role of glycogen synthase kinase 3 β (GSK3β) in mediating the cytotoxic effects of the histone deacetylase inhibitor trichostatin A (TSA) in MCF-7 breast cancer cells.
    Authors: Alao Et al.
    J Cell Biol
  46. The role of protein kinase B/Akt in insulin-induced inactivation of phosphorylase in rat hepatocytes.
    Authors: Aiston Et al.
    Mol Biol Cell
  47. A chaperone-dependent GSK3β transitional intermediate mediates activation-loop autophosphorylation.
    Authors: Lochhead Et al.
    Basic Res Cardiol
  48. Identification of an N-terminal glycogen synthase kinase 3 phosphorylation site which regulates the functional localization of polycystin-2 in vivo and in vitro.
    Authors: Streets Et al.
    Biochim Biophys Acta
  49. Neuronal polarity is regulated by glycogen synthase kinase-3 (GSK-3beta) independently of Akt/PKB serine phosphorylation.
    Authors: Gärtner Et al.
    J Cell Sci
  50. Lithium induces autophagy by inhibiting inositol monophosphatase.
    Authors: Sarkar Et al.
    EMBO J
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