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
* <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.)

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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

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 (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 drug 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

Customer Product Validation

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

Data from [Data independently produced by , , Front Immunol, 2018, 9:2527]

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

Data from [Data independently produced by , , Front Neurosci, 2018, 12:914]

Selleck's Tideglusib has been cited by 27 publications

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
Starvation mediates pancreatic cancer cell sensitivity to ferroptosis via ERK1/2, JNK and changes in the cell mesenchymal state [ Int J Mol Med, 2022, 49(6)84] PubMed: 35514314
The kinase complex mTORC2 promotes the longevity of virus-specific memory CD4+ T cells by preventing ferroptosis [ Nat Immunol, 2021, 10.1038/s41590-021-01090-1] PubMed: 34949833
Evaluating a New Class of AKT/mTOR Activators for HIV Latency-Reversing ActivityEx VivoandIn Vivo [ Journal of Virology, 2021, 95(8)] PubMed: None
Evaluating a New Class of AKT/mTOR Activators for HIV Latency Reversing Activity Ex Vivo and In Vivo [ J Virol, 2021, JVI.02393-20] PubMed: 33536176
Sensitivity of pancreatic cancer cells to chemotherapeutic drugs, signal transduction inhibitors and nutraceuticals can be regulated by WT-TP53 [ Adv Biol Regul, 2021, S2212-4926(20)30091-9] PubMed: 33451973
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] PubMed: 33259812
Bidirectional Regulation between NDRG1 and GSK3β Controls Tumor Growth and Is Targeted by Differentiation Inducing Factor-1 in Glioblastoma. [ Cancer Res, 2020, 80(2):234-248] PubMed: 31723002
Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors. [ JCI Insight, 2020, 5(1)] PubMed: 31821176

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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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