SB 216763

CAS No. 280744-09-4

SB 216763( SB-216763 | SB216763 )

Catalog No. M13854 CAS No. 280744-09-4

SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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25MG 120 In Stock
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Biological Information

  • Product Name
    SB 216763
  • Note
    Research use only, not for human use.
  • Brief Description
    SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.
  • Description
    SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β; displays no significant activity against a panel of 24 other protein kinases; stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes; displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
  • In Vitro
    SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month. SB-216763 inhibits GSK-3 with IC50 of 34 nM. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β.
  • In Vivo
    SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO.
  • Synonyms
    SB-216763 | SB216763
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    GSK-3
  • Recptor
    GSK-3α|GSK-3β
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    280744-09-4
  • Formula Weight
    371.2168
  • Molecular Formula
    C19H12Cl2N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(C(C1=CC=C(Cl)C=C1Cl)=C2C3=CN(C)C4=C3C=CC=C4)NC2=O
  • Chemical Name
    1H-Pyrrole-2,5-dione, 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Coghlan MP, et al. Chem Biol. 2000 Oct;7(10):793-803. 2. Cross DA, et al. J Neurochem. 2001 Apr;77(1):94-102. 3. Lu D, et al. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):3118-23. 4. Gurrieri C, et al. J Pharmacol Exp Ther. 2010 Mar;332(3):785-94.
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