Tideglusib

Catalog No.S2823 Synonyms: NP031112, NP-12

Tideglusib Chemical Structure

Molecular Weight(MW): 334.39

Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.

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1 Customer Review

  • Isoform specificity of different chemical inhibitors of GSK3. Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3′-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.

    PLoS One, 2014, 9(7):e100947. . Tideglusib purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.
Targets
GSK-3β [1]
(Cell-free assay)
60 nM
In vitro

Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons. [1] Tideglusib (2.5 μM) inhibits glutamate-induced glial activation as evidenced by decreased TNF-α and COX-2 expression in rat primary astrocyte or microglial cultures. Tideglusib (2.5 μM) also exerts a potent neuroprotective effect on cortical neurons from glutamate-induced excitotoxicity as evidenced by significant reduction in the number of Annexin-V-positive cells in rat primary astrocyte or microglial cultures. [2]

In vivo Tideglusib (50 mg/kg) injected into the adult male Wistar rats hippocampus dramatically reduces kainic acid-induced inflammation and has a neuroprotective effect in the damaged areas of the hippocampus. [2] Tideglusib (200 mg/kg, oral) results in lower levels of tau phosphorylation, decreased amyloid deposition and plaque-associated astrocytic proliferation, protection of neurons in the entorhinal cortex and CA1 hippocampal subfield against cell death, and prevention of memory deficits in APP/tau double transgenic mice. [3]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
  • Formulation: 26% peg400 (Polyethylene Glycol 400), 15% Chremophor EL and water
  • Dosages: 200 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (197.37 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+corn oil 2.5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 334.39
Formula

C19H14N2O2S

CAS No. 865854-05-3
Storage powder
in solvent
Synonyms NP031112, NP-12

Bio Calculators

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02586935 Recruiting Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario, Canada|St. Michaels Hospital, Toronto|University of Toronto|Anagnostou, Evdokia, M.D. December 2015 Phase 2
NCT01350362 Completed Alzheimers Disease Noscira SA|ICON Clinical Research April 2011 Phase 2
NCT01049399 Completed Progressive Supranuclear Palsy Noscira SA|i3 Research December 2009 --
NCT02858908 Recruiting Myotonic Dystrophy 1 AMO Pharma Limited null Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID