Tideglusib
Based on 7 publication(s) in Google Scholar
Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3βWT (1 h preincubation) and GSK-3βC199A (1 h preincubation), respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.70%
- CAS No.: 865854-05-3
- Formule: C19H14N2O2S
- Masse moléculaire:334.39
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tideglusib
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Mater Today Bio. 2025 Apr 4:32:101730. [Abstract]
- Free Radic Biol Med. 2025 Oct 30:242:275-287. [Abstract]
- Stem Cell Res Ther. 2022 Jun 21;13(1):269. [Abstract]
- Mol Cell Biochem. 2026 Jan 29. [Abstract]
- Biochem Biophys Res Commun. 2021 May 21:554:206-213. [Abstract]
- Int J Clin Exp Pathol. 2017;10(3):3033-3042.
Customer Validation & Images
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IF
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Cell Proliferation/Viability Assay
Activité biologique
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GSK-3β(WT) 5 nM (IC50) |
GSK-3β(C199A) 60 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Vero C1008 | IC50 |
0.67 μM
Compound: 13
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Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
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[PMID: 37244162] |
Incubation of both astrocyte and microglial cultures with Tideglusib (NP031112) completely abrogates the induction of TNF-α and COX-2 expression after glutamate treatment. These effects of NP031112 are not caused by a loss of cell viability, because the 24 h exposure of astrocyte and microglial cells to this TDZD does not modify cell viability[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 865854-05-3
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Appearance Solid
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Masse moléculaire 334.39
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Formule C19H14N2O2S
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Color White to off-white
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SMILES
O=C(N(SC1=O)C2=C3C=CC=CC3=CC=C2)N1CC4=CC=CC=C4
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Synonyms
NP031112
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Mater Today Bio
Bioactive deproteinized bovine bone mineral based on self-assembled albumin nanoparticles promoted bone regeneration via activation of Wnt/β-catenin pathway. [Abstract]2025 Apr 4:32:101730. PMID: 40275954 -
Free Radic Biol Med
7,8-Dihydroxyflavone protects acetaminophen induced liver injury through activating PI3K/Akt/NRF2/GPX4 mediated ferroptosis suppression. [Abstract]2025 Oct 30:242:275-287. PMID: 41173313
Tideglusib purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Oct 30:242:275-287. [Abstract]
HuH7 cells were treated with 7,8-DHF (5 μM), Tideglusib (10 μM) and concentration gradient RSL3 (0-10 μM) for 24 h. Cell viability was measured by CCK-8 assay.
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Stem Cell Res Ther
The metabolism of carbamazepine in humans: steric course of the enzymatic hydrolysis of the 10,11-epoxide. [Abstract]2022 Jun 21;13(1):269. PMID: 3572965 -
Mol Cell Biochem
Bioelectric fields drive pulmonary epithelial proliferation through PI3K/AKT/GSK3β signaling. [Abstract]2026 Jan 29. PMID: 41609898
Tideglusib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2026 Jan 29. [Abstract]
Western blot analysis of p-GSK3β and GSK3β in BEAS-2B and MLE-12 cells treated under indicated conditions: No EF, EFs (100 mV/mm, 2 h), and EFs (100 mV/mm, 2 h)+Tideglusib (TID, 20 µM, 24 h), with quantification of p-GSK3β/GSK3β ratio.
Tideglusib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2026 Jan 29. [Abstract]
Western blot analysis of p-GSK3β and GSK3β in BEAS-2B and MLE-12 cells treated under indicated conditions: No EF, EFs (100 mV/mm, 2 h), and EFs (100 mV/mm, 2 h)+Tideglusib (TID, 20 µM, 24 h), with quantification of p-GSK3β/GSK3β ratio.
Tideglusib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2026 Jan 29. [Abstract]
Immunofluorescence analysis of Ki-67 in MLE-12 cells treated under indicated conditions: No EF, Tideglusib (TID; 20 µM, 24 h), EFs (100 mV/mm, 2 h), and EFs (100 mV/mm, 2 h)+Tideglusib (TID; 20 µM, 24 h), with quantification of Ki-67 positive cells.
Tideglusib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2026 Jan 29. [Abstract]
Immunofluorescence analysis of Ki-67 in BEAS2B cells treated under indicated conditions: No EF, Tideglusib (TID; 20 μM, 24 h), EFs (100 mV/mm, 2 h), and EFs (100 mV/mm, 2 h) + TID(20 μM, 24 h), with quantification of Ki-67 positive cells.
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Biochem Biophys Res Commun
Tideglusib suppresses stem-cell-like features and progression of osteosarcoma by inhibiting GSK-3β/NOTCH1 signaling. [Abstract]2021 May 21:554:206-213. PMID: 33813076 -
Tideglusib purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2017;10(3):3033-3042.
Response of 6 HCC cell lines to 12 antitumor agents (Tideglusib; 0-10μM). The IC50 values were determined by MTS assay and calculated with the aid of GraphPad Prism 5.0 software by nonlinear regression.
Tideglusib purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2017;10(3):3033-3042.
Response of 6 HCC cell lines to 12 antitumor agents (Tideglusib; 0-10μM).
Solvant et solubilité
DMSO : 33.33 mg/mL (99.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Rats[2]
Adult male Wistar rats (8-12 weeks old) are used in this study. Rats (n≥5 per group) are placed into a stereotaxic apparatus. KA (1 μg in 2.5 μL PBS) alone or in combination with Tideglusib (2 ng in 2.5 μL PBS) is injected into the hippocampus. Control animals of the same age are injected with vehicle.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Domínguez JM, et al. Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib. J Biol Chem, 2012, 287(2), 893-90 [Content Brief]
[2]. Luna-Medina R, et al. NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders. J Neurosci, 2007, 27(21), 5766-5776. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.9905 mL | 14.9526 mL | 29.9052 mL | 74.7630 mL |
| 5 mM | 0.5981 mL | 2.9905 mL | 5.9810 mL | 14.9526 mL | |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9905 mL | 7.4763 mL | |
| 15 mM | 0.1994 mL | 0.9968 mL | 1.9937 mL | 4.9842 mL | |
| 20 mM | 0.1495 mL | 0.7476 mL | 1.4953 mL | 3.7381 mL | |
| 25 mM | 0.1196 mL | 0.5981 mL | 1.1962 mL | 2.9905 mL | |
| 30 mM | 0.0997 mL | 0.4984 mL | 0.9968 mL | 2.4921 mL | |
| 40 mM | 0.0748 mL | 0.3738 mL | 0.7476 mL | 1.8691 mL | |
| 50 mM | 0.0598 mL | 0.2991 mL | 0.5981 mL | 1.4953 mL | |
| 60 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2460 mL | |
| 80 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9345 mL |
Tideglusib Related Classifications
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