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TH5487 is a potent 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes.

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TH5487 Chemical Structure

TH5487 Chemical Structure

CAS No. : 2304947-71-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 8 publication(s) in Google Scholar

TH5487 Related Antibodies

Top Publications Citing Use of Products

    TH5487 purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Feb 14;e13418.  [Abstract]

    Th5487 ameliorates renal Renal ischemia-reperfusion injury. Th5487 (30 mg/kg; i.p.; every day for 3 days before the schemia-reperfusion (IR) operation) treatment group shows partial tubular dilation and vacuolar degeneration after IR24h, with a reduced tubular injury score. In comparison, nuclear pyknosis and necrosis of renal tubules are observed in the vehicle group after IR24h (Figure D, E).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TH5487 is a potent 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes[1].

    In Vitro

    TH5487 (5 μM; 1 hour) decreases TNFα- and LPS-induced proinflammatory gene expression to near pretreatment levels[1].
    TH5487 (0-10 μM; 1 hour) perturbs binding of NF-κB to 8-oxoG–containing synthetic DNA in nuclear extracts from MLE 12 or hSAEC cells[1].

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

    TH5487 Related Antibodies

    RT-PCR[1]

    Cell Line: Murine airway epithelial cell line (MLE 12); Diploid human small-airway epithelial cell (hSAECs)
    Concentration: 5 μM
    Incubation Time: 1 hour
    Result: Inhibited proinflammatory gene expression dose-dependently.

    Western Blot Analysis[1]

    Cell Line: Murine airway epithelial cell line (MLE 12); Diploid human small-airway epithelial cell (hSAECs)
    Concentration: 2.5 μM; 5 μM; 10 μM
    Incubation Time: 1 hour
    Result: Decreased p50-p65 and p50-p50 expression in a dose dependent manner.
    In Vivo

    TH5487 (prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours) decreases TNFα or LPS induced the robust recruitment of neutrophils to the airways, and reduces the pulmonary neutrophil count in a time-dependent manner[1].

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

    Animal Model: Eightweek-old female and male BALB/c mice[1]
    Dosage: 8 mg/kg, 15 mg/kg, 30 mg/kg
    Administration: Prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours
    Result: InterruptedTNFα-induced ongoing inflammatory processes.
    Molecular Weight

    541.18

    Formula

    C19H18BrIN4O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N1CCC(N(C2=CC=CC(Br)=C2N3)C3=O)CC1)NC4=CC=C(I)C=C4
    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 : 25 mg/mL (46.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8478 mL 9.2391 mL 18.4781 mL
    5 mM 0.3696 mL 1.8478 mL 3.6956 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.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    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 (3.84 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    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
    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 1.8478 mL 9.2391 mL 18.4781 mL 46.1954 mL
    5 mM 0.3696 mL 1.8478 mL 3.6956 mL 9.2391 mL
    10 mM 0.1848 mL 0.9239 mL 1.8478 mL 4.6195 mL
    15 mM 0.1232 mL 0.6159 mL 1.2319 mL 3.0797 mL
    20 mM 0.0924 mL 0.4620 mL 0.9239 mL 2.3098 mL
    25 mM 0.0739 mL 0.3696 mL 0.7391 mL 1.8478 mL
    30 mM 0.0616 mL 0.3080 mL 0.6159 mL 1.5398 mL
    40 mM 0.0462 mL 0.2310 mL 0.4620 mL 1.1549 mL
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    TH5487 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:

    TH54872304947-71-3TH 5487TH-5487OthersInhibitorinhibitorinhibit

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