TDZD-8
Based on 15 publication(s) in Google Scholar
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.76%
- No. CAS: 327036-89-5
- Fòrmula: C10H10N2O2S
- Peso molecular:222.26
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) TDZD-8
More- Cell Death Differ. 2021 Jan;28(1):337-348. [Abstract]
- J Neuroinflammation. 2023 Feb 24;20(1):49. [Abstract]
- Oncogene. 2024 Sep;43(39):2901-2913. [Abstract]
- Oncogene. 2023 Nov;42(47):3503-3513. [Abstract]
- Oncogene. 2023 Jul;42(30):2297-2314. [Abstract]
- Brain Behav Immun. 2025 Jan:123:229-243. [Abstract]
- Eur J Med Chem. 2017 Jul 28:135:370-381. [Abstract]
- Int Immunopharmacol. 2025 Sep 10:165:115526. [Abstract]
- Int Immunopharmacol. 2025 Jun 17:158:114817. [Abstract]
- Exp Neurol. 2025 Aug:390:115262. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2020 Apr 20;52(4):363-370. [Abstract]
- Hum Exp Toxicol. 2021 Sep;40(9):1584-1597. [Abstract]
- Exp Cell Res. 2019 Oct 15;383(2):111557. [Abstract]
- Exp Lung Res. 2025;51(1):79-92. [Abstract]
- Research Square Print. 2023 Feb 7.
Customer Validation & Images
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IF
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WB
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In Vivo Imaging
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IHC
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IHC
Actividad biológica
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GSK-3β 2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
20 μM
Compound: TDZD-8
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Antiproliferative activity against human A2780 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells measured after 48 hrs by MTT assay
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[PMID: 28460311] |
| Vero C1008 | IC50 |
0.67 μM
Compound: 15; TDZD-8
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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] |
TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells. TDZD8 (10 μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells. Furthermore, TDZD8 (10 μM) reduces mTOR phosphorylation levels at the S2448 site. In addition, TDZD8 (10 μM) induces LKB1 nuclear-cytoplasm translocation[3].
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.
Chemical Information
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No. CAS 327036-89-5
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Appearance Solid
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Peso molecular 222.26
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Fòrmula C10H10N2O2S
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Color White to light yellow
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SMILES
O=C(N1CC2=CC=CC=C2)N(C)SC1=O
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Synonyms
GSK-3β Inhibitor I; NP 01139
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
RPS23RG1 modulates tau phosphorylation and axon outgrowth through regulating p35 proteasomal degradation. [Abstract]2021 Jan;28(1):337-348. PMID: 32908202 -
J Neuroinflammation
Human umbilical cord-derived mesenchymal stem cell transplantation supplemented with curcumin improves the outcomes of ischemic stroke via AKT/GSK-3β/β-TrCP/Nrf2 axis. [Abstract]2023 Feb 24;20(1):49. PMID: 36829224
TDZD-8 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Feb 24;20(1):49. [Abstract]
Representative images of immunofluorescence analysis of Nrf2 expression in microglia treated with the AKT inhibitor MK2206 (5 μM，6 h), the GSK3β activator sodium nitroprusside (SNP, 100 μM， 6h), and the GSK3β inhibitor TDZD-8 (5 μM，6 h). Nrf2 (red), nuclei (blue).
TDZD-8 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Feb 24;20(1):49. [Abstract]
Representative western blots and quantitative data for the expression of Nrf2 in the nucleus and the downstream proteins of Nrf2 pathway, including HO-1 and NQO1, with different treatments (MK2206: 5 μM，6 h; SNP: 100 μM， 6h; TDZD-8: 5 μM，6 h).
TDZD-8 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Feb 24;20(1):49. [Abstract]
Nrf2 knockout abolished neurological function improvement mediated by combined curcumin-hUC-MSC treatment. TTC-stained brain sections (A) and quantitative analysis (B) showed the decreased infarct volume with combined therapy in MCAO mice (MK2206, SNP or TDZD-8 :5 mg/kg， intraperitoneally，3 consecutive days after MCAO).
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Oncogene
2024 Sep;43(39):2901-2913. PMID: 39164523 -
Oncogene
D-mannose induces TFE3-dependent lysosomal degradation of EGFR and inhibits the progression of NSCLC. [Abstract]2023 Nov;42(47):3503-3513. PMID: 37845392 -
Oncogene
GSK3β-driven SOX2 overexpression is a targetable vulnerability in esophageal squamous cell carcinoma. [Abstract]2023 Jul;42(30):2297-2314. PMID: 37349645 -
Brain Behav Immun
Astrocyte-neuron communication through the complement C3-C3aR pathway in Parkinson's disease. [Abstract]2025 Jan:123:229-243. PMID: 39288893 -
Eur J Med Chem
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. [Abstract]2017 Jul 28:135:370-381. PMID: 28460311 -
Int Immunopharmacol
Aβ impairs bone vascular homeostasis in APP/PS1 mice via disrupting the mitochondrial fission-efferocytosis axis in macrophages. [Abstract]2025 Sep 10:165:115526. PMID: 40934542 -
Int Immunopharmacol
Monotropein synergizes with methotrexate to attenuate synovial inflammation in adjuvant-induced arthritis mice and fibroblast-like synoviocyte via GSK-3β. [Abstract]2025 Jun 17:158:114817. PMID: 40349405 -
Exp Neurol
4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione rescues oligodendrocytes ferroptosis leading to myelin loss and ameliorates neuronal injury facilitating memory in neonatal hypoxic-ischemic brain damage. [Abstract]2025 Aug:390:115262. PMID: 40246011 -
Acta Biochim Biophys Sin (Shanghai)
Inhibition of glycogen synthase kinase 3β improves cognitive function in aged mice by upregulating claudin presences in cerebral endothelial cells. [Abstract]2020 Apr 20;52(4):363-370. PMID: 32141492
TDZD-8 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Apr 20;52(4):363-370. [Abstract]
Aged mice have abnormal BBB permeability in the hippocampus. Fluorescence signals of 40 kDa dextran in the mouse hippocampus. DAPI labeled the nuclei (blue), CD31 labeled endothelial cells (green, Fluor 488), and dextran is stained in red (Texas red).
TDZD-8 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Apr 20;52(4):363-370. [Abstract]
Aged mice have abnormal BBB permeability in the hippocampus. Immunofluorescence signals of claudin1 in the hippocampus. DAPI labeled the nuclei (blue), CD31 labeled endothelial cells (green, Fluor488), the target proteins claudin1 is stained in red (Fluor594).
TDZD-8 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Apr 20;52(4):363-370. [Abstract]
Aged mice have abnormal BBB permeability in the hippocampus. Immunofluorescence signals of claudin5 in the hippocampus. DAPI labeled the nuclei (blue), CD31 labeled endothelial cells (green, Fluor488), the target proteins claudin5 is stained in red (Fluor594).
TDZD-8 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Apr 20;52(4):363-370. [Abstract]
Aged mice exhibit enhanced inflammation and increased expression of GSK protein in the hippocampus. Representative western blots of total and phosphorylated GSK-3β protein.
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Hum Exp Toxicol
Gastrodin protects against high glucose-induced cardiomyocyte toxicity via GSK-3β-mediated nuclear translocation of Nrf2. [Abstract]2021 Sep;40(9):1584-1597. PMID: 33764184 -
Exp Cell Res
Taurine protects against myelin damage of sciatic nerve in diabetic peripheral neuropathy rats by controlling apoptosis of schwann cells via NGF/Akt/GSK3β pathway. [Abstract]2019 Oct 15;383(2):111557. PMID: 31415759 -
Exp Lung Res
PM2.5 induces ferroptosis in chronic obstructive pulmonary diseases via the GSK-3β/NRF2 pathway. [Abstract]2025;51(1):79-92. PMID: 40889519 -
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (449.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (11.25 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.25 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocolo
GSK-3 activity is assayed in 50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, and 1 mM EDTA buffer, at 37°C, in the presence of 15 μM GS-1 (substrate), 15 μM [γ-32P]ATP in a final volume of 12 μL. After 20 min incubation at 37°C, 4 μL aliquots of the supernatant are spotted onto 2×2 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed four times (for at least 10 min each time) in 1% phosphoric acid. The dried filters are transferred into scintillation vials, and the radioactivity is measured in a liquid scintillation counter. Blank values are subtracted, and the GSK-3β activity is expressed in picomoles of phosphate incorporated in GS-1 per 20 min or in percentage of maximal activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Apomorphine hydrochloride is administered (0.5 mg/kg). L-dopa (25 mg/kg) plus benserazide-HCl (6.25 mg/kg) are given once-daily. TDZD8, a non-ATP competitive inhibitor of GSK-3β, is dissolved in 10% DMSO and is administered i.p. (TDZD8-L group, 1 mg/kg; TDZD8-H group, 2 mg/kg, respectively) 30 min prior to L-dopa intake for 3 weeks. (±)-1-Phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride (SKF38393), a D1 Dopamine receptor agonist, is dissolved in saline and is administered i.p. (SKF38393-L group, 5 mg/kg; SKF38393-H group, 10 mg/kg, respectively) 30 min prior to L-dopa intake for 3 weeks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Martinez A, et al. First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J Med Chem. 2002 Mar 14;45(6):1292-9. [Content Brief]
[2]. Xie CL, et al. Inhibition of Glycogen Synthase Kinase-3β (GSK-3β) as potent therapeutic strategy to ameliorates L-dopa-induced dyskinesia in 6-OHDA parkinsonian rats. Sci Rep. 2016 Mar 21;6:23527. [Content Brief]
[3]. Sun A, et al. GSK-3β controls autophagy by modulating LKB1-AMPK pathway in prostate cancer cells. Prostate. 2016 Feb;76(2):172-83. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4992 mL | 22.4962 mL | 44.9924 mL | 112.4809 mL |
| 5 mM | 0.8998 mL | 4.4992 mL | 8.9985 mL | 22.4962 mL | |
| 10 mM | 0.4499 mL | 2.2496 mL | 4.4992 mL | 11.2481 mL | |
| 15 mM | 0.2999 mL | 1.4997 mL | 2.9995 mL | 7.4987 mL | |
| 20 mM | 0.2250 mL | 1.1248 mL | 2.2496 mL | 5.6240 mL | |
| 25 mM | 0.1800 mL | 0.8998 mL | 1.7997 mL | 4.4992 mL | |
| 30 mM | 0.1500 mL | 0.7499 mL | 1.4997 mL | 3.7494 mL | |
| 40 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.8120 mL | |
| 50 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2496 mL | |
| 60 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8747 mL | |
| 80 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4060 mL | |
| 100 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL |
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