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SB 216763

Catalog #: 1616
75 Citations Datasheet
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1616/1
SB 216763 | CAS No. 280744-09-4 | GSK-3 Inhibitors
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Description: Potent, selective GSK-3 inhibitor

Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione

Purity: ≥98%

Product Details
Citations (75)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

SB 216763 is a 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:
371.22
Formula:
C19H12Cl2N2O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
280744-09-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Frat2 mediates the oncogenic activation of Rac by MLL fusions.
    Walf-Vorderwulbecke V, de Boer J, Horton S, van Amerongen R, Proost N, Berns A, Williams O
    Blood, 2012;120(24):4819-28.
  2. Pharmacological inhibition of GSK-3 in a guinea pig model of LPS-induced pulmonary inflammation: I. Effects on lung remodeling and pathology.
    Baarsma H, Bos S, Meurs H, Visser K, Smit M, Schols A, Langen R, Kerstjens H, Gosens R
    Respir Res, 2013;14(0):113.
  3. Effects of kinesin-5 inhibition on dendritic architecture and microtubule organization.
    Kahn O, Sharma V, Gonzalez-Billault C, Baas P
    Mol Biol Cell, 2015;26(1):66-77.
  4. Wnt activation by wild type and mutant myocilin in cultured human trabecular meshwork cells.
    Shen X, Ying H, Yue B
    PLoS ONE, 2012;7(9):e44902.
  5. PLK1 stabilizes a MYC-dependent kinase network in aggressive B cell lymphomas
    Y Ren, C Bi, X Zhao, T Lwin, C Wang, J Yuan, AS Silva, BD Shah, B Fang, T Li, JM Koomen, H Jiang, JC Chavez, L Pham, PR Sudalagunt, L Wan, X Wang, WS Dalton, LC Moscinski, KH Shain, J Vose, JL Cleveland, EM Sotomayor, K Fu, J Tao
    J. Clin. Invest., 2018;0(0):.
  6. Glycogen synthase kinase-3 controls IL-10 expression in CD4(+) effector T-cell subsets through epigenetic modification of the IL-10 promoter.
    Hill E, Ng T, Burton B, Oakley C, Malik K, Wraith D
    Eur J Immunol, 2015;45(4):1103-15.
  7. H(2)O(2) Production Downstream of FLT3 Is Mediated by p22phox in the Endoplasmic Reticulum and Is Required for STAT5 Signalling.
    Woolley JF, Naughton R, Stanicka J, Gough DR, Bhatt L, Dickinson BC, Chang CJ, Cotter TG
    PLoS ONE, 2012;7(7):e34050.
  8. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.
    Kirby et al.
    PLoS One, 2012;7:e39329
  9. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.
    Cross et al.
    J.Neurochem., 2001;77:94
  10. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
    Coghlan et al.
    Chem.Biol., 2000;7:793
  11. 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
  12. Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival.
    Liang and Chuang
    J.Biol.Chem., 2006;282:3904

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Citations for SB 216763

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

75 Citations: Showing 1 - 10

  1. Inhibition of cardiomyocyte Sprouty1 protects from cardiac ischemia-reperfusion injury.
    Authors: Alakoski Et al.
    Basic Res Cardiol  2019;114:7
  2. Sexual dimorphism in PAR2-dependent regulation of primitive colonic cells.
    Authors: Noguerol Et al.
    Biol Sex Differ  2019;10:47
  3. Aberrant regulation of the GSK-3β/NRF2 axis unveils a novel therapy for adrenoleukodystrophy.
    Authors: Ranea-Robles Et al.
    EMBO Mol Med  2018;10
  4. Subcellular localization of the FLT3-ITD oncogene plays a significant role in the production of NOX- and p22(phox)-derived reactive oxygen species in acute myeloid leukemia.
    Authors: Moloney Et al.
    Leuk Res  2017;52:34
  5. WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling.
    Authors: Abedini Et al.
    FASEB J  2016;30:1534
  6. GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling.
    Authors: Stretton Et al.
    Biomed Res Int  2015;470:207
  7. 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  2015;45:1103
  8. Glycogen synthase kinase-3 (GSK3) inhibition induces prosurvival autophagic signals in human pancreatic cancer cells.
    Authors: Marchand Et al.
    Dev Cell  2015;290:5592
  9. Effects of kinesin-5 inhibition on dendritic architecture and microtubule organization.
    Authors: Kahn Et al.
    Mol Biol Cell  2015;26:66
  10. Phosphorylation and SCF-mediated degradation regulate CREB-H transcription of metabolic targets.
    Authors: Barbosa Et al.
    Proc Natl Acad Sci U S A  2015;26:2939
  11. Morphine Reduces Myocardial Infarct Size via Heat Shock Protein 90 in Rodents.
    Authors: Small Et al.
    J Biol Chem  2015;2015:129612
  12. Apelin-13 protects the heart against ischemia-reperfusion injury through the RISK-GSK-3β-mPTP pathway.
    Authors: Yang Et al.
    Mol Biol Cell  2015;11:1065
  13. Targeting β-arrestin2 in the treatment of L-DOPA-induced dyskinesia in Parkinson's disease.
    Authors: Urs Et al.
    Biochem J  2015;112:E2517
  14. Extracellular α-synuclein leads to microtubule destabilization via GSK-3β-dependent Tau phosphorylation in PC12 cells.
    Authors: Gassowska Et al.
    PLoS One  2014;9:e94259
  15. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.
    Authors: Naujok Et al.
    BMC Res Notes  2014;7:273
  16. Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by Ins.
    Authors: Kuo Et al.
    J Lipid Res  2014;55:919
  17. 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  2014;289:11007
  18. β-arrestin2/miR-155/GSK3β regulates transition of 5'-azacytizine-induced Sca-1-positive cells to cardiomyocytes.
    Authors: Zhao Et al.
    J Cell Biol  2014;18:1562
  19. Inhibiting glycogen synthase kinase-3 mitigates the hematopoietic acute radiation syndrome in mice.
    Authors: Lee Et al.
    Radiat Res  2014;181:445
  20. Tristetraprolin mediates radiation-induced TNF-α production in lung macrophages.
    Authors: Ray Et al.
    PLoS One  2013;8:e57290
  21. Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division.
    Authors: Robertson Et al.
    Mol Cancer  2013;2:472
  22. Preventing p38 MAPK-mediated MafA degradation ameliorates β-cell dysfunction under oxidative stress.
    Authors: Khattabi and Sharma
    Hum Mol Genet  2013;27:1078
  23. N-cadherin specifies first asymmetry in developing neurons.
    Authors: Gärtner Et al.
    Mol Med  2012;31:1893
  24. Inhibition of GSK3 attenuates amphetamine-induced hyperactivity and sensitization in the mouse.
    Authors: Enman and Unterwald
    Neuro Oncol  2012;231:217
  25. Death receptors DR6 and TROY regulate brain vascular development.
    Authors: Tam Et al.
    Eur J Immunol  2012;22:403
  26. Glycogen synthase kinase 3β inhibitors protect hippocampal neurons from radiation-induced apoptosis by regulating MDM2-p53 pathway.
    Authors: Thotala Et al.
    Cell Death Differ  2012;19:387
  27. Inhibition of GSK3 abolishes bacterial-induced periodontal bone loss in mice.
    Authors: Adamowicz Et al.
    Mol Cell  2012;18:1190
  28. Involvement of the glycogen synthase kinase-3 signaling pathway in TBI pathology and neurocognitive outcome.
    Authors: Dash Et al.
    PLoS One  2011;6:e24648
  29. Li suppresses astrogliogenesis by neural stem and progenitor cells by inhibiting STAT3 pathway independently of glycogen synthase kinase 3 beta.
    Authors: Zhu Et al.
    PLoS One  2011;6:e23341
  30. Inhibition of adipocytogenesis by canonical WNT signaling in human mesenchymal stem cells.
    Authors: Shen Et al.
    Exp Cell Res  2011;317:1796
  31. 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  2011;300:L910
  32. GSK3β inactivation induces apoptosis of leukemia cells by repressing the function of c-Myb.
    Authors: Zhou Et al.
    J Cell Mol Med  2011;22:3533
  33. The role of glycogen synthase kinase 3 in regulating IFN-β-mediated IL-10 production.
    Authors: Wang Et al.
    J Immunol  2011;186:675
  34. 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  2011;186:5217
  35. Glycogen synthase kinase 3β inhibition enhances repair of DNA double-strand breaks in irradiated hippocampal neurons.
    Authors: Yang Et al.
    Diabetologia  2011;13:459
  36. A new class of molecular targeted radioprotectors: GSK-3beta inhibitors.
    Authors: Thotala Et al.
    Int J Radiat Oncol Biol Phys  2010;76:557
  37. GSK3 regulates the expressions of human and mouse c-Myb via different mechanisms.
    Authors: Kitagawa Et al.
    Cell Div  2010;5:27
  38. Phosphorylation-dependent regulation of PSF by GSK3 controls CD45 alternative splicing.
    Authors: Heyd
    Mol Cell  2010;40:126
  39. 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  2010;285:31427
  40. Frizzled1 is a marker of inflammatory macrophages, and its ligand Wnt3a is involved in reprogramming Mycobacterium tuberculosis-infected macrophages.
    Authors: Neumann Et al.
    FASEB J  2010;24:4599
  41. DISC1 regulates new neuron development in the adult brain via modulation of AKT-mTOR signaling through KIAA1212.
    Authors: Kim Et al.
    Neuron  2009;63:761
  42. Polycomb limits the neurogenic competence of neural precursor cells to promote astrogenic fate transition.
    Authors: Hirabayashi Et al.
    Neuron  2009;63:600
  43. GSK3beta regulates differentiation and growth arrest in glioblastoma.
    Authors: Korur Et al.
    PLoS One  2009;4:e7443
  44. Evidence for involvement of ERK, PI3K, and RSK in induction of Bcl-2 by valproate.
    Authors: Creson Et al.
    J Mol Neurosci  2009;37:123
  45. 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  2009;33:193
  46. p38 MAPK is a major regulator of MafA protein stability under oxidative stress.
    Authors: Kondo Et al.
    Mol Endocrinol  2009;23:1281
  47. 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  2009;183:4475
  48. Toll-like receptor-mediated production of IL-1Ra is negatively regulated by GSK3 via the MAPK ERK1/2.
    Authors: Rehani Et al.
    J Immunol  2009;182:547
  49. Phosphorylation of CLASP2 by GSK-3beta regulates its interaction with IQGAP1, EB1 and microtubules.
    Authors: Watanabe Et al.
    J Cell Sci  2009;122:2969
  50. Runx expression is mitogenic and mutually linked to Wnt activity in blastula-stage sea urchin embryos.
    Authors: Robertson Et al.
    PLoS One  2008;3:e3770
  51. Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion.
    Authors: Gross Et al.
    Am J Physiol Heart Circ Physiol  2008;294:H1497
  52. Loss of PINK1 function affects development and results in neurodegeneration in zebrafish.
    Authors: Anichtchik Et al.
    J Neurosci  2008;28:8199
  53. 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  2008;283:35337
  54. Antigenic experience dictates functional role of glycogen synthase kinase-3 in human CD4+ T cell responses.
    Authors: Garcia Et al.
    J Immunol  2008;181:8363
  55. IFN-beta production by TLR4-stimulated innate immune cells is negatively regulated by GSK3-beta.
    Authors: Wang Et al.
    J Immunol  2008;181:6797
  56. A rational mechanism for combination treatment of Huntington's disease using Li and rapamycin.
    Authors: Sarkar Et al.
    Hum Mol Genet  2008;17:170
  57. 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  2008;103:464
  58. Glycogen synthase kinase 3 regulates N-MthD.-aspartate receptor channel trafficking and function in cortical neurons.
    Authors: Chen Et al.
    Mol Pharmacol  2007;72:40
  59. Diabetes abolishes morphine-induced cardioprotection via multiple pathways upstream of glycogen synthase kinase-3beta.
    Authors: Gross Et al.
    Diabetes  2007;56:127
  60. Activation of glycogen synthase kinase-3 inhibits long-term potentiation with synapse-associated impairments.
    Authors: Zhu Et al.
    J Neurosci  2007;27:12211
  61. Phosphatidylinositol 3-kinase regulation of gastrin-releasing peptide-induced cell cycle progression in neuroblastoma cells.
    Authors: Ishola Et al.
    Biol Open  2007;1770:927
  62. GEF-H1 modulates localized RhoA activation during cytokinesis under the control of mitotic kinases.
    Authors: Birkenfeld Et al.
    Dev Cell  2007;12:699
  63. 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  2007;120:2935
  64. Polarity reveals intrinsic cell chirality.
    Authors: Xu Et al.
    Proc Natl Acad Sci U S A  2007;104:9296
  65. Histone deacetylase inhibitor, trichostatin A induces ubiquitin-dependent cyclin D1 degradation in MCF-7 breast cancer cells.
    Authors: Alao Et al.
    Mol Cancer  2006;5:8
  66. The cyclin D1 proto-oncogene is sequestered in the cytoplasm of mammalian cancer cell lines.
    Authors: Alao Et al.
    Mol Cancer  2006;5:7
  67. 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  2006;5:40
  68. The role of protein kinase B/Akt in Ins-induced inactivation of phosphorylase in rat hepatocytes.
    Authors: Aiston Et al.
    Mol Biol Cell  2006;49:174
  69. The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta.
    Authors: Gross Et al.
    Am J Physiol Heart Circ Physiol  2006;291:H827
  70. A chaperone-dependent GSK3β transitional intermediate mediates activation-loop autophosphorylation.
    Authors: Lochhead Et al.
    Basic Res Cardiol  2006;24:627
  71. 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  2006;15:1465
  72. Neuronal polarity is regulated by glycogen synthase kinase-3 (GSK-3beta) independently of Akt/PKB serine phosphorylation.
    Authors: Gärtner Et al.
    J Cell Sci  2006;119:3927
  73. Li induces autophagy by inhibiting inositol monophosphatase.
    Authors: Sarkar Et al.
    EMBO J  2005;170:1101
  74. Opioid-induced cardioprotection occurs via glycogen synthase kinase beta inhibition during reperfusion in intact rat hearts.
    Authors: Gross Et al.
    Circ Res  2004;94:960
  75. Li antagonizes DA-dependent behaviors mediated by an AKT/glycogen synthase kinase 3 signaling cascade.
    Authors: Beaulieu Et al.
    Proc Natl Acad Sci U S A  2004;101:5099

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