Tideglusib

Catalog No.S2823 Batch:S282304

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Technical Data

Formula

C19H14N2O2S
Molecular Weight 334.39 CAS No. 865854-05-3
Solubility (25°C)* In vitro DMSO 8 mg/mL (23.92 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; this compound 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.

This compound (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. It (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.

This compound (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.

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[4]
  • Cell lines

    Miapaca2 cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of this compound for 24 h.
Animal Study:

[3]
  • Animal Models

    Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.

  • Dosages

    200 mg/kg

  • Administration

    Oral gavage

References

  • https://pubmed.ncbi.nlm.nih.gov/22102280/
  • https://pubmed.ncbi.nlm.nih.gov/17522320/
  • https://pubmed.ncbi.nlm.nih.gov/19523516/
  • https://pubmed.ncbi.nlm.nih.gov/35514314/

Customer Product Validation

<p>(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.</p>

, , Ann Neurol, 2016, doi: 10.1002/ana.24633

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.

Data from [ , , Front Immunol, 2018, 9:2527 ]

(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).

Data from [ , , Oncotarget, 2016, 7(12):13575-86 ]

(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.

Data from [ , , Front Neurosci, 2018, 12:914 ]

Selleck's Tideglusib Has Been Cited by 35 Publications

TRAF6 inhibits colorectal cancer metastasis through regulating selective autophagic CTNNB1/β-catenin degradation and is targeted for GSK3B/GSK3β-mediated phosphorylation and degradation [ Autophagy, September 2019, 1506-1522] PubMed: 30806153
Targeted strategy by curcumin and tideglusib biomimetic nano-systems alleviates oxidative stress and inflammation under ischemic stroke [ Drug Delivery, November 25, 2025, 1-15] PubMed: 41292262
A Selective GSK3β Inhibitor, Tideglusib, Decreases Intermittent Access and Binge Ethanol Self-Administration in C57BL/6J Mice [ Addiction Biology, May 2025, e70044] PubMed: 40390305
Preclinical testing of the glycogen synthase kinase-3β inhibitor tideglusib for rhabdomyosarcoma [ Oncotarget, June 16, 2017, 62976-62983] PubMed: 28968964
Bidirectional Regulation between NDRG1 and GSK3β Controls Tumor Growth and Is Targeted by Differentiation Inducing Factor-1 in Glioblastoma [ Cancer Research, January 15, 2020, 234-248] PubMed: 31723002
Tideglusib Rescues Neurite Pathology of SPG11 iPSC Derived Cortical Neurons [ Frontiers in Neuroscience, December 6, 2018, 914] PubMed: 30574063
A Selective GSK3β Inhibitor, Tideglusib, Decreases Intermittent Access and Binge Ethanol Self-Administration in C57BL/6J Mice [ Addict Biol, 2025, 30(5):e70044] PubMed: 40390305
The TRIM4 E3 ubiquitin ligase degrades TPL2 and is modulated by oncogenic KRAS [ Cell Rep, 2024, 43(9):114667] PubMed: 39178114
Activity and inhibition of the SARS-CoV-2 Omicron nsp13 R392C variant using RNA duplex unwinding assays [ SLAS Discov, 2024, S2472-5552(24)00007-8] PubMed: 38301954
SYK coordinates neuroprotective microglial responses in neurodegenerative disease [ Cell, 2022, 185(22):4135-4152.e22] PubMed: 36257314

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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