Home / GSK-3 Inhibitors / SB 415286

SB 415286

Catalog #: 1617
27 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1617/10
1617/50
SB 415286 | CAS No. 264218-23-7 | GSK-3 Inhibitors
1 Image
Description: Potent, selective GSK-3 inhibitor

Chemical Name: 3-[(3-Chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione

Purity: ≥99%

Product Details
Citations (27)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

SB 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.

Technical Data

M.Wt:
359.73
Formula:
C16H10ClN3O5
Solubility:
Soluble to 25 mM in ethanol and to 50 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
264218-23-7

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

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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

  1. mTOR-dependent phosphorylation controls TFEB nuclear export.
    Authors: Napolitano Et al.
    Nat Commun  2018;9:3312
  2. Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
    Authors: Liddell Et al.
    J Neuroinflammation  2016;13:49
  3. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation.
    Authors: Wang Et al.
    Sci Rep  2015;5:8566
  4. 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
  5. GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling.
    Authors: Stretton Et al.
    J Biol Chem  2015;470:207
  6. Tau reduction prevents Aβ-induced axonal transport deficits by blocking activation of GSK3β.
    Authors: Vossel Et al.
    Biochem J  2015;209:419
  7. GSK3β Inhibition Promotes Synaptogenesis in Drosophila and Mammalian Neurons.
    Authors: Cuesto Et al.
    PLoS One  2015;10:e0118475
  8. Sequential dosing in chemosensitization: targeting the PI3K/Akt/mTOR pathway in neuroblastoma.
    Authors: Westhoff Et al.
    PLoS One  2014;8:e83128
  9. 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
  10. Inhibiting glycogen synthase kinase-3 mitigates the hematopoietic acute radiation syndrome in mice.
    Authors: Lee Et al.
    Radiat Res  2014;181:445
  11. Tristetraprolin mediates radiation-induced TNF-α production in lung macrophages.
    Authors: Ray Et al.
    PLoS One  2013;8:e57290
  12. 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
  13. Sidestream smoke exposure increases the susceptibility of airway epithelia to adenoviral infection.
    Authors: Sharma Et al.
    PLoS One  2012;7:e49930
  14. 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
  15. Glycogen synthase kinase 3β inhibition enhances repair of DNA double-strand breaks in irradiated hippocampal neurons.
    Authors: Yang Et al.
    Nature  2011;13:459
  16. 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
  17. A new class of molecular targeted radioprotectors: GSK-3beta inhibitors.
    Authors: Thotala Et al.
    Int J Radiat Oncol Biol Phys  2010;76:557
  18. Molecular imaging of glycogen synthase kinase-3beta and casein kinase-1alpha kinases.
    Authors: Nyati Et al.
    Anal Biochem  2010;405:246
  19. 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
  20. The mood stabilizers valproic acid and Li enhance mesenchymal stem cell migration via distinct mechanisms.
    Authors: Tsai Et al.
    Neuropsychopharmacology  2010;35:2225
  21. Phosphorylation of CLASP2 by GSK-3beta regulates its interaction with IQGAP1, EB1 and microtubules.
    Authors: Watanabe Et al.
    J Cell Sci  2009;122:2969
  22. Microtubule stabilization specifies initial neuronal polarization.
    Authors: Witte Et al.
    J Cell Biol  2008;180:619
  23. Cdc42 regulates cofilin during the establishment of neuronal polarity.
    Authors: Garvalov Et al.
    J Neurosci  2007;27:13117
  24. 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
  25. 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
  26. 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
  27. 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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