2. Neuronal Signaling Autophagy
  3. OGA Autophagy
  4. Thiamet G

Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.

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

CAS No. : 1009816-48-1

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Customer Review

Based on 48 publication(s) in Google Scholar

Thiamet G Related Antibodies

Top Publications Citing Use of Products

48 Publications Citing Use of MCE Thiamet G

Gel Electrophoresis
IP
Apoptosis Analysis

    Thiamet G purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2025 Oct 6.  [Abstract]

    Analysis of UGDH glycosylation in HEK293T cells overexpressing Flag-tagged UGDH under co-transfection of HA-OGT or TMG treatment (50 μM; 48 h).

    Thiamet G purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Nov 28:e2407519.  [Abstract]

    HUCCT1-TRCs or RBE-TRCs were treated with TM (2.5 μg mL−1) or TG (Thiamet G) (50 μm) for 48 h.

    Thiamet G purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 11;12(1):2672.  [Abstract]

    MDA-MB-231 and HCC1806 cells were treated with TM (2.5 μg/ml), Thiamet G (50 μM), and PUGNAc (100 μM) for 24 h.

    Thiamet G purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 11;12(1):2672.  [Abstract]

    The indicated cell lines were treated with N-linked glycosylation inhibitors TM (2.5 μg/ml), SW (5 μg/ml), and DMJ (10 μg/ml), or O-linked glycosylation inhibitors Thiamet G (50 μM) and PUGNAc (100 μM) for 24 h.

    Thiamet G purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Jul:43:101994.  [Abstract]

    Representative blots of O-GlcNAc modified G6PDH in the mouse hearts with indicated treatments,mice were treated by intraperitoneal injection with alloxan (ALX, 100 mg/kg; Sigma) or Thiamet-G (TMG, 20 mg/kg; MCE) at 6 h before cardiac I/R surgery

    Thiamet G purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jun 1;10(16):7178-7192.  [Abstract]

    TMG reduced gemcitabine induced apoptosis in L3.6pl while show no difference in TBO368. Cells were treated as indicated for 48 h and 72 h, in L3.6pl and TBO368, respectively. TMG (Thiamet G), 5 µM.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.

    IC50 & Target

    Ki: 20 nM (Human OGA)[1]
    Cellular Effect
    Cell Line Type Value Description References
    PC-12 EC50
    30 nM
    Compound: thiamet-G
    Induction of O-GlcNAc level in NGF-differentiated rat PC12 cells after 24 hrs by densitometric analysis
    Induction of O-GlcNAc level in NGF-differentiated rat PC12 cells after 24 hrs by densitometric analysis
    		[PMID: 18587388]
    In Vitro

    Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, and p38 but not phosphorylation of Akt[2]. Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau and alters the microtubule dynamics[3].

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

    Thiamet G Related Antibodies
    In Vivo

    Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues[1].
    Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner[2].

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

    248.30

    Formula

    C9H16N2O4S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O[C@H]1[C@H](O)[C@@]2([H])N=C(NCC)S[C@@]2([H])O[C@@H]1CO
    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 : 233.33 mg/mL (939.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 50 mg/mL (201.37 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0274 mL 20.1369 mL 40.2739 mL
    5 mM 0.8055 mL 4.0274 mL 8.0548 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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: ≥ 2.08 mg/mL (8.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 50 mg/mL (201.37 mM); Clear solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.99%

    SDS (393 KB)

    COA (248 KB) HNMR (250 KB) RP-HPLC (206 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [3]

    All enzymatic assays are performed in triplicate at 37°C using 4-methylumbelliferyl N-acetyl-β-d-glucosaminide dehydrate as substrate. 1 nM of purified OGA is incubated with the compounds for 5 min, and then 0.2 mM of the substrate is added. The liberation of 4-methylumbellifery is monitored by kinetic reading at excitation/emission 355/460 nm using a Tecan M200 plate in a mode of 60 s/cycle and 15 cycles in total.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    Jurkat cells are seeded at 6000 cells/well in a 96-well plate, and 12 h later, cells are treated with compounds for the indicated time. Cell viability is determined by XTT assay.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    For the Thiamet G dose dependence study, six 23-day-old male C57BL/6 mice receive single intraperitoneal injections of either 0, 10, 20, 100, 200, or 500 mg/kg of Thiamet G dissolved in PBS and then are euthanized 8 h later to evaluate the O-GlcNAc levels in different tissues (brain, liver, muscle, and knee). The time of sacrifice is chosen on the basis of previously published data on Thiamet G in rodents, which demonstrates that the peak level of O-GlcNAc proteins following administration of the drug is achieved after 8-10 h. Tissues are collected immediately after sacrifice, flash-frozen in liquid nitrogen, and stored at −80°C until required for use.

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 4.0274 mL 20.1369 mL 40.2739 mL 100.6847 mL
    5 mM 0.8055 mL 4.0274 mL 8.0548 mL 20.1369 mL
    10 mM 0.4027 mL 2.0137 mL 4.0274 mL 10.0685 mL
    15 mM 0.2685 mL 1.3425 mL 2.6849 mL 6.7123 mL
    20 mM 0.2014 mL 1.0068 mL 2.0137 mL 5.0342 mL
    25 mM 0.1611 mL 0.8055 mL 1.6110 mL 4.0274 mL
    30 mM 0.1342 mL 0.6712 mL 1.3425 mL 3.3562 mL
    40 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5171 mL
    50 mM 0.0805 mL 0.4027 mL 0.8055 mL 2.0137 mL
    60 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6781 mL
    80 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2586 mL
    100 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Thiamet G 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:

    Thiamet G1009816-48-1OGAAutophagyO-GlcNAc hydrolaseO-GlcNAcaseInhibitorinhibitorinhibit

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