Art. -Nr.: HY-11012

TDZD-8

(Synonyms: GSK-3β Inhibitor I; NP 01139)

15 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.76%
CAS. Nr.: 327036-89-5
Formel: C₁₀H₁₀N₂O₂S
Molecular Weight:222.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TDZD-8 Chemical Structure

CAS. Nr.: 327036-89-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target^[1]

GSK-3β

2 μM (IC₅₀)

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	20 μM Compound: TDZD-8	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	[PMID: 28460311]
Vero C1008	IC₅₀	0.67 μM Compound: 15; TDZD-8	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	[PMID: 37244162]

In Vitro

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.

In Vivo

TDZD-8 (TDZD8, 1 or 2 mg/kg, i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals. TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia. Moreover, TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa. The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 327036-89-5
Appearance Solid
Molecular Weight 222.26
Formel C₁₀H₁₀N₂O₂S
Color White to light yellow
SMILES

O=C(N1CC2=CC=CC=C2)N(C)SC1=O
Synonyms

GSK-3β Inhibitor I; NP 01139
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (15)

All IFWBIn Vivo ImagingIHC

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Journal Impact Factor

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).
Oncogene

Alternative splicing of ALDOA confers tamoxifen resistance in breast cancer. [Abstract]

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.
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
Research Square Print

2023 Feb 7.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.4992 mL

22.4962 mL

44.9924 mL

5 mM

0.8998 mL

4.4992 mL

8.9985 mL

10 mM

0.4499 mL

2.2496 mL

4.4992 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[1]

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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

TDZD-8

15 Cited Publications

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TDZD-8

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Targeted Diversity Library

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Human Metabolite Library

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Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) TDZD-8

Alle GSK-3 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TDZD-8 Related Classifications

HY-11012 Related Classifications