Tideglusib

For research use only.

Catalog No.S2823 Synonyms: NP031112, NP-12

19 publications

Tideglusib Chemical Structure

CAS No. 865854-05-3

Tideglusib (NP031112, NP-12) 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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Selleck's Tideglusib has been cited by 19 publications

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Biological Activity

Description Tideglusib (NP031112, NP-12) 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]

Assay
Methods Test Index PMID
Western blot
KDM1A / Nestin / OCT4 / CD133 / Tuj-1; 

PubMed: 27501329     


GSC11 cells were treated with 2.5 µM or 5 µM tideglusib for 36 h, and cell lysates were assessed by immunoblotting. 

27501329
Growth inhibition assay
Cell viability; 

PubMed: 27501329     


(e) GSC11 and GSC20 cells were treated with different concentration of tideglusib for 7d. IC50 values for each cell line were calculated using the GraphPad Prism 6 software (mean ± s.e.m., n=3 independent experiments). (f) GSC11 and GSC20 cells were treated with dimethyl sulfoxide (DMSO), temozolomide (TMZ; 100 µM), tideglusib (2.5 µM), or TMZ plus tideglusib for the indicated times, and cell proliferation was assessed by XTT assays (mean ± s.e.m., n=3 independent experiments, paired Student’s t-test). P values were analyzed by comparing TMZ or tideglusib along versus the combination of the two and shown. 

27501329
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]
- Collapse
  • Animal Models: Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
  • Dosages: 200 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 8 mg/mL warmed (23.92 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.
2.5mg/mL

* 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
Smiles C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02586935 Completed Drug: Tideglusib|Other: Placebo Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario Canada|St. Michael''s Hospital Toronto|University of Toronto|Anagnostou Evdokia M.D. February 10 2016 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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Frequently Asked Questions

  • Question 1:

    I want to deliver S2823 via i.p. injection, can you suggest one?

  • Answer:

    This compound can be dissolved in 4% DMSO+corn oil at 2.5 mg/ml clearly. This is the highest concentration, since its solubility in DMSO is pretty low.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID