For research use only.
Catalog No.S2823 Synonyms: NP031112, NP-12
CAS No. 865854-05-3
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.
Selleck's Tideglusib has been cited by 17 publications
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(A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs.
Ann Neurol, 2016, doi: 10.1002/ana.24633. Tideglusib purchased from Selleck.
BV-2 cells were pretreated with NP-12 (an inhibitor of GSK-3β, 2.5 μM) for 4 h, following which they were treated with PLD for 1 h. After cells were harvested, the protein expression of GSK-3β, p-GSK-3βSer9 (D), and Nucleosol-Nrf2 (E) was measured via Western blotting.
Front Immunol, 2018, 9:2527. Tideglusib purchased from Selleck.
(C) and Western blotting (D) analysis showed treatment with GSK3β inhibitors TWS119 (10 μM) and Tideglusib (1 μM) for 24 hours suppressed E-cadherin expression in FGF19 knockdown MHCC97H cells. All error bars in this figure represent S.E.M. (n = 3, **P < 0.01).
Oncotarget, 2016, 7(12):13575-86. Tideglusib purchased from Selleck.
(A) Merged confocal images of SPG11 and CTRL neurons generated from iPSCs and co-immunostained for βIII-tubulin (Tuj-1) and cleaved-caspase3 (cCasp3). Scale bar = 20 μm. (B) Representative images of TUJ-1 stained SPG11 and control neurons.
Front Neurosci, 2018, 12:914. Tideglusib purchased from Selleck.
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.
Purity & Quality Control
Choose Selective GSK-3 Inhibitors
|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.|
Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons.  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. 
|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.  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. |
|In vitro||DMSO||8 mg/mL warmed (23.92 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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Frequently Asked Questions
I want to deliver S2823 via i.p. injection, can you suggest one?
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.