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  2. GSK-3
  3. TDZD-8

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

Cat. No.: HY-11012 Purity: 99.54%
Handling Instructions

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
10 mM * 1  mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TDZD-8 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Mar 6. pii: gmaa002. 

    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 MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Mar 6. pii: gmaa002. 

    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 MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Mar 6. pii: gmaa002. 

    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 MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2020 Mar 6. pii: gmaa002. 

    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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    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].

    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].

    Molecular Weight

    222.26

    Formula

    C₁₀H₁₀N₂O₂S

    CAS No.

    327036-89-5

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (449.92 mM)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    TDZD-8GSK-3β Inhibitor INP 01139TDZD8TDZD 8NP01139NP-01139GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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