SB 216763

Cat. No. 1616

SB 216763 C19H12Cl2N2O2 [280744-09-4]

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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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

Soluble to 75 mM in DMSO
>98 %
Store at RT

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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Kirby et al (2012) Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One 7 e39329. PMID: 22745733.

Gurrieri et al (2010) 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. J.Pharmacol.Exp.Ther. 332 785. PMID: 19959748.

Liang and Chuang (2006) Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 282 3904. PMID: 17148450.

Cross et al (2001) Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 77 94. PMID: 11279265.

Coghlan et al (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 7 793. PMID: 11033082.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SB 216763 include:

Barbosa et al (2015) Phosphorylation and SCF-mediated degradation regulate CREB-H transcription of metabolic targets. Proc Natl Acad Sci U S A 26 2939. PMID: 26108621.

Hill et al (2015) Glycogen synthase kinase-3 controls IL-10 expression in CD4(+) effector T-cell subsets through epigenetic modification of the IL-10 promoter. Arch Med Sci 45 1103. PMID: 25627813.

Kahn et al (2015) Effects of kinesin-5 inhibition on dendritic architecture and microtubule organization. Mol Biol Cell 26 66. PMID: 25355946.

Marchand et al (2015) Glycogen synthase kinase-3 (GSK3) inhibition induces prosurvival autophagic signals in human pancreatic cancer cells. Dev Cell 290 5592. PMID: 25561726.

Small et al (2015) Morphine Reduces Myocardial Infarct Size via Heat Shock Protein 90 in Rodents. J Biol Chem 2015 129612. PMID: 26413502.

Stretton et al (2015) GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling. Biomed Res Int 470 207. PMID: 26348909.

Urs et al (2015) Targeting β-arrestin2 in the treatment of L-DOPA-induced dyskinesia in Parkinson's disease. Biochem J 112 E2517. PMID: 25918399.

Yang et al (2015) Apelin-13 protects the heart against ischemia-reperfusion injury through the RISK-GSK-3β-mPTP pathway. Mol Biol Cell 11 1065. PMID: 26528352.

Acevedo et al (2014) Phosphorylation of amyloid precursor protein at threonine 668 is essential for its copper-responsive trafficking in SH-SY5Y neuroblastoma cells. Mol Endocrinol 289 11007. PMID: 24610780.

Gassowska et al (2014) Extracellular α-synuclein leads to microtubule destabilization via GSK-3β-dependent Tau phosphorylation in PC12 cells. PLoS One 9 e94259. PMID: 24722055.

Kuo et al (2014) Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by insulin. J Lipid Res 55 919. PMID: 24565756.

Lee et al (2014) Inhibiting glycogen synthase kinase-3 mitigates the hematopoietic acute radiation syndrome in mice. Radiat Res 181 445. PMID: 24720754.

Zhao et al (2014) β-arrestin2/miR-155/GSK3β regulates transition of 5'-azacytizine-induced Sca-1-positive cells to cardiomyocytes. J Cell Biol 18 1562. PMID: 24974728.

Khattabi and Sharma (2013) Preventing p38 MAPK-mediated MafA degradation ameliorates β-cell dysfunction under oxidative stress. Hum Mol Genet 27 1078. PMID: 23660596.

Ray et al (2013) Tristetraprolin mediates radiation-induced TNF-α production in lung macrophages. PLoS One 8 e57290. PMID: 23468959.

Robertson et al (2013) Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division. Mol Cancer 2 472. PMID: 23789095.

Adamowicz et al (2012) Inhibition of GSK3 abolishes bacterial-induced periodontal bone loss in mice. Mol Cell 18 1190. PMID: 22847803.

Enman and Unterwald (2012) Inhibition of GSK3 attenuates amphetamine-induced hyperactivity and sensitization in the mouse. Neuro Oncol 231 217. PMID: 22649795.

Gärtner et al (2012) N-cadherin specifies first asymmetry in developing neurons. Mol Med 31 1893. PMID: 22354041.

Tam et al (2012) Death receptors DR6 and TROY regulate brain vascular development. Eur J Immunol 22 403. PMID: 22340501.

Thotala et al (2012) Glycogen synthase kinase 3β inhibitors protect hippocampal neurons from radiation-induced apoptosis by regulating MDM2-p53 pathway. Cell Death Differ 19 387. PMID: 21738215.

Baarsma et al (2011) Glycogen synthase kinase-3 regulates cigarette smoke extract- and IL-1β-induced cytokine secretion by airway smooth muscle. Am J Physiol Lung Cell Mol Physiol 300 L910. PMID: 21421749.

Dash et al (2011) Involvement of the glycogen synthase kinase-3 signaling pathway in TBI pathology and neurocognitive outcome. PLoS One 6 e24648. PMID: 21935433.

Shen et al (2011) Inhibition of adipocytogenesis by canonical WNT signaling in human mesenchymal stem cells. Exp Cell Res 317 1796. PMID: 21640723.

Wang et al (2011) The role of glycogen synthase kinase 3 in regulating IFN-β-mediated IL-10 production. J Immunol 186 675. PMID: 21160051.

Wang et al (2011) Convergence of the mammalian target of rapamycin complex 1- and glycogen synthase kinase 3-β-signaling pathways regulates the innate inflammatory response. J Immunol 186 5217. PMID: 21422248.

Yang et al (2011) Glycogen synthase kinase 3β inhibition enhances repair of DNA double-strand breaks in irradiated hippocampal neurons. Diabetologia 13 459. PMID: 21398658.

Zhou et al (2011) GSK3β inactivation induces apoptosis of leukemia cells by repressing the function of c-Myb. J Cell Mol Med 22 3533. PMID: 21795403.

Fong et al (2010) Tumor-supportive and osteoclastogenic changes induced by breast cancer-derived factors are reversed by inhibition of {gamma}-secretase. J Biol Chem 285 31427. PMID: 20679341.

Neumann et al (2010) Frizzled1 is a marker of inflammatory macrophages, and its ligand Wnt3a is involved in reprogramming Mycobacterium tuberculosis-infected macrophages. FASEB J 24 4599. PMID: 20667980.

Garcia et al (2009) c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells. J Immunol 183 4475. PMID: 19734233.

Hu et al (2009) GSK3 inhibitors show benefits in an Alzheimer's disease (AD) model of neurodegeneration but adverse effects in control animals. Neurobiol Dis 33 193. PMID: 19038340.

Kondo et al (2009) p38 MAPK is a major regulator of MafA protein stability under oxidative stress. Mol Endocrinol 23 1281. PMID: 19407223.

Rehani et al (2009) Toll-like receptor-mediated production of IL-1Ra is negatively regulated by GSK3 via the MAPK ERK1/2. J Immunol 182 547. PMID: 19109187.

Watanabe et al (2009) Phosphorylation of CLASP2 by GSK-3beta regulates its interaction with IQGAP1, EB1 and microtubules. J Cell Sci 122 2969. PMID: 19638411.

Anichtchik et al (2008) Loss of PINK1 function affects development and results in neurodegeneration in zebrafish. J Neurosci 28 8199. PMID: 18701682.

Clifford et al (2008) Novel regulation of vascular endothelial growth factor-A (VEGF-A) by transforming growth factor (beta)1: requirement for Smads, (beta)-CATENIN, AND GSK3(beta). J Biol Chem 283 35337. PMID: 18952601.

Cohen et al (2008) Acidosis, oxygen, and interference with mitochondrial permeability transition pore formation in the early minutes of reperfusion are critical to postconditioning's success. Behav Brain Res 103 464. PMID: 18626679.

Garcia et al (2008) Antigenic experience dictates functional role of glycogen synthase kinase-3 in human CD4+ T cell responses. J Immunol 181 8363. PMID: 19050253.

Sarkar et al (2008) A rational mechanism for combination treatment of Huntington's disease using lithium and rapamycin. Hum Mol Genet 17 170. PMID: 17921520.

Wang et al (2008) IFN-beta production by TLR4-stimulated innate immune cells is negatively regulated by GSK3-beta. J Immunol 181 6797. PMID: 18981097.

Ishola et al (2007) Phosphatidylinositol 3-kinase regulation of gastrin-releasing peptide-induced cell cycle progression in neuroblastoma cells. Biol Open 1770 927. PMID: 17379415.

Lin et al (2007) GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis. J Cell Sci 120 2935. PMID: 17666435.

Xu et al (2007) Polarity reveals intrinsic cell chirality. Proc Natl Acad Sci U S A 104 9296. PMID: 17517645.

Aiston et al (2006) The role of protein kinase B/Akt in insulin-induced inactivation of phosphorylase in rat hepatocytes. Mol Biol Cell 49 174. PMID: 16341839.

Alao et al (2006) 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. J Cell Biol 5 40. PMID: 17018141.

Gärtner et al (2006) Neuronal polarity is regulated by glycogen synthase kinase-3 (GSK-3beta) independently of Akt/PKB serine phosphorylation. J Cell Sci 119 3927. PMID: 16954147.

Lochhead et al (2006) A chaperone-dependent GSK3β transitional intermediate mediates activation-loop autophosphorylation. Basic Res Cardiol 24 627. PMID: 17188038.

Streets et al (2006) Identification of an N-terminal glycogen synthase kinase 3 phosphorylation site which regulates the functional localization of polycystin-2 in vivo and in vitro. Biochim Biophys Acta 15 1465. PMID: 16551655.

Sarkar et al (2005) Lithium induces autophagy by inhibiting inositol monophosphatase. EMBO J 170 1101. PMID: 16186256.

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Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, inhibits, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK, Tocris Bioscience, Glycogen Synthase Kinase 3 Inhibitor products

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