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

M.Wt:
371.22
Formula:
C19H12Cl2N2O2
Solubility:
Soluble to 75 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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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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.

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

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

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.

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

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.

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.

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.

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.

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.

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.

Do you know of a great paper that uses SB 216763 from Tocris? If so please let us know.show all ▼show less ▲

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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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