Tideglusib

Catalog No.S2823

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.

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Tideglusib Chemical Structure

Tideglusib Chemical Structure
Molecular Weight: 334.39

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

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)
IC50 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]
Features

Protocol(Only for 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.

Animal Study: [3]

Animal Models Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
Formulation 26% peg400 (Polyethylene Glycol 400), 15% Chremophor EL and water
Dosages 200 mg/kg
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Domínguez JM, et al. J Biol Chem, 2012, 287(2), 893-90

[2] Luna-Medina R, et al. J Neurosci, 2007, 27(21), 5766-5776.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02586935 Recruiting Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation  ...more Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario, Canada|St. Michaels Hospital, Toronto|University of Toronto|Anagnostou, Evdokia, M.D. December 2015 Phase 2
NCT01350362 Completed Alzheimers Disease Noscira SA|ICON Clinical Research April 2011 Phase 2
NCT01049399 Completed Progressive Supranuclear Palsy Noscira SA|i3 Research December 2009 --

Chemical Information

Download Tideglusib SDF
Molecular Weight (MW) 334.39
Formula

C19H14N2O2S

CAS No. 865854-05-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NP031112, NP-12
Solubility (25°C) * In vitro DMSO 66 mg/mL warming (197.37 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 4% DMSO+corn oil 2.5mg/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.
Chemical Name 1,2,4-Thiadiazolidine-3,5-dione, 2-(1-naphthalenyl)-4-(phenylmethyl)-

Tech Support

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