LY2090314 | Wnt/ß-Catenin pathway activator/GSK-3 inhibitor

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Wnt/ß-catenin pathway activator. LY2090314 (603288-22-8) is a highly potent (IC50 = 1.5 nM GSK-3α; 0.9 nM GSK-3ß) and selective inhibitor of glycogen synthase-3-kinase (GSK-3).1,2  It stabilized ß-catenin levels and elevated expression of Axin2 leading to tumor growth delays in A375 melanoma xenografts.2 LY2090314 significantly reduced growth in multiple neuroblastoma cell lines.3 It inhibited growth and induced apoptosis in osimertinib-resistant lung cancer cells, specifically those with a mesenchymal phenotype.4

References/Citations:

  1. Engler et al. (2004), Substituted 3-imidazo[1,2-a]pyridine-3-yl-4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1=hi]indol-7-yl)pyrrole-2,5-diones as and potent inhibitors of glycogen synthase-3-kinase; J. Med. Chem. 47 3934
  2. Atkinson et al. (2015), Activating the Wnt/ß-Catenin Pathway for the Treatment of Melanoma – Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3; PLoS One 10 e0125028
  3. Kunnimalaiyaan et al. (2018), Antiproliferative and apoptotic effect of LY2090314, a GSK-3 inhibitor, in neuroblastoma in vitro BMC Cancer 18 560
  4. Fukuda et al. (2020), Glycogen synthase kinase-3 inhibition overcomes epithelial-mesenchymal transition-associated resistance to Osimertinib in EGFR-mutant lung cancer; Cancer Sci. 111 2374
603288-22-8, GSK-3 inhibitor, LY 2090314, LY2090314, LY2090314 supplier, Potent GSK-3 inhibitor, Wnt pathway activator, Wnt/ß-catenin pathway activator

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Wnt/ß-catenin pathway activator. LY2090314 (603288-22-8) is a highly potent (IC50 = 1.5 nM GSK-3α; 0.9 nM GSK-3ß) and selective inhibitor of glycogen synthase-3-kinase (GSK-3).1,2  It stabilized ß-catenin levels and elevated expression of Axin2 leading to tumor growth delays in A375 melanoma xenografts.2 LY2090314 significantly reduced growth in multiple neuroblastoma cell lines.3 It inhibited growth and induced apoptosis in osimertinib-resistant lung cancer cells, specifically those with a mesenchymal phenotype.4

References/Citations:

  1. Engler et al. (2004), Substituted 3-imidazo[1,2-a]pyridine-3-yl-4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1=hi]indol-7-yl)pyrrole-2,5-diones as and potent inhibitors of glycogen synthase-3-kinase; J. Med. Chem. 47 3934
  2. Atkinson et al. (2015), Activating the Wnt/ß-Catenin Pathway for the Treatment of Melanoma – Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3; PLoS One 10 e0125028
  3. Kunnimalaiyaan et al. (2018), Antiproliferative and apoptotic effect of LY2090314, a GSK-3 inhibitor, in neuroblastoma in vitro BMC Cancer 18 560
  4. Fukuda et al. (2020), Glycogen synthase kinase-3 inhibition overcomes epithelial-mesenchymal transition-associated resistance to Osimertinib in EGFR-mutant lung cancer; Cancer Sci. 111 2374

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