Tideglusib (NP031112)

Catalog No.S2823 Synonyms: NP-12

For research use only.

Tideglusib (NP031112, NP-12) 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 (NP031112) Chemical Structure

CAS No. 865854-05-3

Selleck's Tideglusib (NP031112) has been cited by 24 publications

Purity & Quality Control

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Biological Activity

Description Tideglusib (NP031112, NP-12) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y MliySpVv[3Srb36gZZN{[Xl? NYDseoZxOTBidV2= M4rVcVEhcHK| NIewdmJKdmirYnn0bY9vKG:oIFfTT{0{[mW2YTDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBidXmub3nkJIJmfGFiKEK1JJRwKDN3KTCtbY5lfWOnZDD0c5hq[2m2eTDheEAyOCC3TTDwdoUucW6ldXLheIVlKG[xcjCxJIhzeyCkZX\vdoUh[W27bH;p[EBj\XSjIDiyOUB1dyB|NTmgZYRlcXSrb36gZY5lKG2nYYP1doVlKGGodHXyJFczKGi{czDwc5N1KEGkZYThNlUuOzViYXTkbZRqd25iYomgUXRVKGG|c3H5 M2rrWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkC4OVIzLz5{OUKwPFUzOjxxYU6=
SH-SY5Y NFzTSWJHfW6ldHnvckBie3OjeR?= MnnqN|AhfU1? NULod2Y6OSCqcoO= NV:xUowyUW6qaXLpeIlwdiCxZjDHV2suO2KndHGgbY4hcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[W27bH;p[EBj\XSjIDiyOUB1dyB|NTmgMYlv\HWlZXSgeI95cWOrdImgZZQhOzBidV2gdJJmNWmwY4XiZZRm\CCob4KgNUBpenNiYnXmc5JmKGGveXzvbYQh[mW2YTCoNlUhfG9iM{WpJIFl\Gm2aX;uJIFv\CCvZXHzeZJm\CCjZoTldkA4OiCqcoOgdI9{fCCDYnX0ZVI2NTN3IHHk[Il1cW:wIHL5JG1VXCCjc4PhfS=> M4rWelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkC4OVIzLz5{OUKwPFUzOjxxYU6=
Assay
Methods Test Index PMID
Western blot KDM1A / Nestin / OCT4 / CD133 / Tuj-1 27501329
Growth inhibition assay Cell viability 27501329
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)

Animal Research:[3]
  • Animal Models: Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
  • Dosages: 200 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

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.

2.5mg/mL

Chemical Information

Molecular Weight 334.39
Formula

C19H14N2O2S

CAS No. 865854-05-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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|Unity Health Toronto|University of Toronto|Anagnostou Evdokia M.D. February 10 2016 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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