TDZD-8 (Synonyms: GSK-3β Inhibitor I; NP 01139)

Name: TDZD-8
Brand: MedChemExpress
SKU: HY-11012
Rating: 5.0 (15 reviews)

Cat. No.: HY-11012 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

TDZD-8 Chemical Structure

CAS No. : 327036-89-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 56	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 56	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 23	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 15 publication(s) in Google Scholar

11 Publications Citing Use of MCE TDZD-8

IHC

: 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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GSK-3 GSK-3α GSK-3β

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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]

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.

Molecular Weight

222.26

Formula

C₁₀H₁₀N₂O₂S

CAS No.

327036-89-5

Appearance

Solid

Color

White to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (282 KB) SDS (418 KB)

COA (251 KB) HNMR (233 KB) LCMS (262 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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

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

TDZD-8 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TDZD-8327036-89-5GSK-3β Inhibitor I NP 01139TDZD8TDZD 8NP01139NP 01139NP-01139GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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TDZD-8 (Synonyms: GSK-3β Inhibitor I; NP 01139)

Customer Review

TDZD-8 Related Antibodies

11 Publications Citing Use of MCE TDZD-8

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All GSK-3 Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

TDZD-8 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TDZD-8 Related Classifications

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