Home PI3K/Akt/mTOR GSK-3 inhibitor - COVID-19 inhibitor Tideglusib For research use only.

Tideglusib

Synonyms: NP031112, NP-12

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.

Tideglusib Chemical Structure

Tideglusib Chemical Structure

CAS No. 865854-05-3

Purity & Quality Control

Tideglusib Related Products

Signaling Pathway

GSK-3 Signaling Pathways

GSK-3 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y Function assay 10 uM 1 hrs Inhibition of GSK-3beta in human SH-SY5Y cells assessed as reduction in amyloid beta (25 to 35) -induced toxicity at 10 uM pre-incubated for 1 hrs before amyloid beta (25 to 35) addition and measured after 72 hrs post Abeta25-35 addition by MTT assay 29208522
SH-SY5Y Function assay 30 uM 1 hrs Inhibition of GSK-3beta in human SH-SY5Y cells assessed as reduction in amyloid beta (25 to 35) -induced toxicity at 30 uM pre-incubated for 1 hrs before amyloid beta (25 to 35) addition and measured after 72 hrs post Abeta25-35 addition by MTT assay 29208522
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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
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]
Kinase Assay Binding Experiments with Radiolabeled Tideglusib
[35S]Tideglusib (207 Bq/nmol) at 55 μM is incubated with 5 μM GSK-3β for 1 h at 25 °C in 315 μL of 50 mM Tris-HCl, pH 7.5, containing 150 mM NaCl and 0.1 mM EGTA. The incubation is extended for another 30 min after having added 35 μL of the same buffer with or without 100 mM DTE. Finally, a third 40-μL aliquot of each original sample is mixed with 10 μL of denaturing electrophoresis sample buffer without reducing agents, and 35 μL of this mixture is loaded onto a 10% polyacrylamide gel and subjected to SDS-PAGE, followed by fluorography of the dried gel.
Cell Research Cell lines Miapaca2 cells
Concentrations 5 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot KDM1A / Nestin / OCT4 / CD133 / Tuj-1 27501329
Growth inhibition assay Cell viability 27501329
In Vivo
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]
Animal Research Animal Models Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
Dosages 200 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02586935 Completed
Autism Spectrum Disorders
Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario Canada|Unity Health Toronto|University of Toronto|Anagnostou Evdokia M.D.
 February 10 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 334.39 Formula

C19H14N2O2S
CAS No. 865854-05-3 SDF Download Tideglusib SDF
Smiles C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 1 mg/mL ( (2.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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