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ProductsBack/SB216763 [280744-09-4]
Chemical Structure
Chemical Structure
Chemical Structure

SB216763 [280744-09-4]

Research Use Only
AG-CR1-3659
AdipoGen Life Sciences
CAS Number280744-09-4
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight371.2
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    SB216763 [280744-09-4]
  • Delivery Days Customer
    10
  • CAS Number
    280744-09-4
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C19H12Cl2N2O2
  • Molecular Weight
    371.2
  • Scientific Description
    Chemical. CAS: 280744-09-4. Formula: C19H12Cl2N2O2. MW: 371.2. Synthetic. Potent and selective cell permeable, ATP-competitive inhibitor of GSK3alpha with an IC50 value of 34nM (and similar potency for GSK3beta). DYRK1A inhibitor (IC50=0.8microM). Stimulates glycogen synthesis in liver cells and induces beta-catenin-dependent gene transcription. Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. Anticancer agent with antiproliferative activity. Reduces pulmonary inflammation and fibrosis in a mouse model. Shown to delay preconditioning, reduces infarct size and prevents cardiac ischemia. Promotes pluripotency in mouse embryonic stem cells. Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis and inflammation. - Potent and selective cell permeable, ATP-competitive inhibitor of GSK3alpha with an IC50 value of 34nM (and similar potency for GSK3beta). DYRK1A inhibitor (IC50=0.8microM). Stimulates glycogen synthesis in liver cells and induces beta-catenin-dependent gene transcription. Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. Anticancer agent with antiproliferative activity. Reduces pulmonary inflammation and fibrosis in a mouse model. Shown to delay preconditioning, reduces infarct size and prevents cardiac ischemia. Promotes pluripotency in mouse embryonic stem cells. Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis and inflammation.
  • SMILES
    O=C(N1)C(C2=CN(C)C3=C2C=CC=C3)=C(C4=C(Cl)C=C(Cl)C=C4)C1=O
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    51202000

References

  • Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription: M.P. Coghlan, et al.; Chem. Biol. 7, 793 (2000)
  • Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death: D.A. Cross, et al.; J. Neurochem. 77, 94 (2001)
  • GSK3 inhibitors: development and therapeutic potential: P. Cohen & M. Goedert; Nat. Rev. Drug Discov. 3, 479 (2004)
  • The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007)
  • Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival: M.H. Liang & D.M. Chuang; J. Biol. Chem. 282, 3904 (2007)
  • Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion: E.R. Gross, et al.; Am. J. Physiol. Heart Circ. Physiol. 294, H1497 (2008)
  • 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: C. Gurrieri, et al.; J. Pharmacol. Exp. Ther. 332, 785 (2010)
  • Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells: L.A. Kirby, et al.; PLoS One 7, e39329 (2012)
  • GSK-3 inhibitor inhibits cell proliferation and induces apoptosis in human osteosarcoma cells: H. Nishimura, et al.; Oncol. Rep. 35, 2348 (2016)