2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. TDZD-8

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

Cat. No.: HY-11012 Purity: 99.81%
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

TDZD-8 Chemical Structure

CAS No. : 327036-89-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 56 In-stock
Solution
10 mM * 1 mL in DMSO USD 56 In-stock
Solid
1 mg USD 23 In-stock
5 mg USD 50 In-stock
10 mg USD 66 In-stock
25 mg USD 99 In-stock
50 mg USD 165 In-stock
100 mg USD 275 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

TDZD-8 Related Antibodies

Top Publications Citing Use of Products

    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.

    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. 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 claudin5 in the hippocampus. DAPI labeled the nuclei (blue), CD31 labeled endothelial cells (green, Fluor488), the target proteins claudin5 is stained in red (Fluor594).

    View All GSK-3 Isoform Specific Products:

    View All Isoforms
    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)

    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.

    TDZD-8 Related Antibodies
    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.
    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
    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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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%

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

    Handling Instructions (2659 KB)
    References
    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

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    TDZD-8
    Cat. No.:
    HY-11012
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.