Chemical Name: 3-[(3-Chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Biological ActivitySB 415286 is a potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 31 nM for GSK-3α); competes with ATP. Has minimal activity against 24 other protein kinases (IC50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.
Cross et al.
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Coghlan et al.
Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival.
Liang and Chuang
Citations for SB 415286
The citations listed below are publications that use Tocris products. Selected citations for SB 415286 include:
27 Citations: Showing 1 - 10
mTOR-dependent phosphorylation controls TFEB nuclear export.
Authors: Napolitano Et al.
Nat Commun 2018;9:3312
Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
Authors: Liddell Et al.
J Neuroinflammation 2016;13:49
Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation.
Authors: Wang Et al.
Sci Rep 2015;5:8566
Resveratrol regulates naïve CD 8+ T-cell proliferation by upregulating IFN-γ-induced tryptophanyl-tRNA synthetase expression.
Authors: Noh Et al.
BMB Rep 2015;48:283
GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling.
Authors: Stretton Et al.
J Biol Chem 2015;470:207
Tau reduction prevents Aβ-induced axonal transport deficits by blocking activation of GSK3β.
Authors: Vossel Et al.
Biochem J 2015;209:419
GSK3β Inhibition Promotes Synaptogenesis in Drosophila and Mammalian Neurons.
Authors: Cuesto Et al.
PLoS One 2015;10:e0118475
Sequential dosing in chemosensitization: targeting the PI3K/Akt/mTOR pathway in neuroblastoma.
Authors: Westhoff Et al.
PLoS One 2014;8:e83128
Phosphorylation of amyloid precursor protein at threonine 668 is essential for its copper-responsive trafficking in SH-SY5Y neuroblastoma cells.
Authors: Acevedo Et al.
Hum Mol Genet 2014;289:11007
Inhibiting glycogen synthase kinase-3 mitigates the hematopoietic acute radiation syndrome in mice.
Authors: Lee Et al.
Radiat Res 2014;181:445
Tristetraprolin mediates radiation-induced TNF-α production in lung macrophages.
Authors: Ray Et al.
PLoS One 2013;8:e57290
Anti-dengue virus nonstructural protein 1 antibodies cause NO-mediated endothelial cell apoptosis via ceramide-regulated glycogen synthase kinase-3β and NF-κB activation.
Authors: Chen Et al.
J Immunol 2013;191:1744
Sidestream smoke exposure increases the susceptibility of airway epithelia to adenoviral infection.
Authors: Sharma Et al.
PLoS One 2012;7:e49930
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
Glycogen synthase kinase 3β inhibition enhances repair of DNA double-strand breaks in irradiated hippocampal neurons.
Authors: Yang Et al.
GSK-3β inhibition promotes cell death, apoptosis, and in vivo tumor growth delay in neuroblastoma Neuro-2A cell line.
Authors: Dickey Et al.
J Neurooncol 2011;104:145
A new class of molecular targeted radioprotectors: GSK-3beta inhibitors.
Authors: Thotala Et al.
Int J Radiat Oncol Biol Phys 2010;76:557
Molecular imaging of glycogen synthase kinase-3beta and casein kinase-1alpha kinases.
Authors: Nyati Et al.
Anal Biochem 2010;405:246
Glycogen Synthase Kinase 3 (GSK-3) influences epithelial barrier function by regulating occludin, claudin-1 and E-cadherin expression.
Authors: Severson Et al.
Neuro Oncol 2010;397:592
The mood stabilizers valproic acid and Li enhance mesenchymal stem cell migration via distinct mechanisms.
Authors: Tsai Et al.
Phosphorylation of CLASP2 by GSK-3beta regulates its interaction with IQGAP1, EB1 and microtubules.
Authors: Watanabe Et al.
J Cell Sci 2009;122:2969
Microtubule stabilization specifies initial neuronal polarization.
Authors: Witte Et al.
J Cell Biol 2008;180:619
Cdc42 regulates cofilin during the establishment of neuronal polarity.
Authors: Garvalov Et al.
J Neurosci 2007;27:13117
Phosphatidylinositol 3-kinase regulation of gastrin-releasing peptide-induced cell cycle progression in neuroblastoma cells.
Authors: Ishola Et al.
Biochem Biophys Res Commun 2007;1770:927
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
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
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
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