2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. GSK717

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.

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CAS No. : 1595278-21-9

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Customer Review

Based on 8 publication(s) in Google Scholar

GSK717 Related Antibodies

Top Publications Citing Use of Products

    GSK717 purchased from MedChemExpress. Usage Cited in: Drug Resist Updat. 2023 Nov:71:101005.

    GSK717 (50 μM) impaired the expression of NF-κB and ABC transporters in pancreatic cancer cells.

    GSK717 purchased from MedChemExpress. Usage Cited in: Drug Resist Updat. 2023 Nov:71:101005.

    GSK717 (50 μM) increased GEM-induced apoptosis of pancreatic cancer cells.

    GSK717 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2022 Oct 12;30(10):1435-1449.e9.  [Abstract]

    GSK717 (10 μg/g; i.p.; 1 d). Body weight change, colon length, and intestinal barrier permeability of mice with DSS-induced colitis were indicated by FITC-dextran permeability.

    GSK717 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2022 Oct 12;30(10):1435-1449.e9.  [Abstract]

    GSK717 (10 μg/g; i.p.; 1 d). Levels of cytokines (TNF-a, IFN-g, IL-17, and IL-16) in serum of mice with DSS-induced colitis.

    GSK717 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2022 Oct 12;30(10):1435-1449.e9.  [Abstract]

    GSK717 (10 μg/g; i.p.; 1 d). Representative PCNA staining of colonic sections of mice with DSS-induced colitis.

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    NLRP3 NLRP1 NOD1 NOD2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T IC50
    0.4 μM
    Compound: 26, GSK717
    Inhibition of NOD1 (unknown origin) expressed in HEK293T cells coexpressing NF-kappaB driven luciferase reporter gene by HTS primary assay
    Inhibition of NOD1 (unknown origin) expressed in HEK293T cells coexpressing NF-kappaB driven luciferase reporter gene by HTS primary assay
    		[PMID: 24707857]
    In Vitro

    GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP[1].

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

    GSK717 Related Antibodies
    Molecular Weight

    452.55

    Formula

    C28H28N4O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=C2C(CCC2)=C1)CN3C4=CC=CC=C4N=C3CCN(C)C(C5=CC=CC=C5)=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 : 250 mg/mL (552.43 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 2.2097 mL 11.0485 mL 22.0970 mL
    5 mM 0.4419 mL 2.2097 mL 4.4194 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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 (4.60 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 (4.60 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Dosing volume
    (per animal)

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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:
    %
    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: 99.93%

    SDS (396 KB)

    COA (256 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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 2.2097 mL 11.0485 mL 22.0970 mL 55.2425 mL
    5 mM 0.4419 mL 2.2097 mL 4.4194 mL 11.0485 mL
    10 mM 0.2210 mL 1.1049 mL 2.2097 mL 5.5243 mL
    15 mM 0.1473 mL 0.7366 mL 1.4731 mL 3.6828 mL
    20 mM 0.1105 mL 0.5524 mL 1.1049 mL 2.7621 mL
    25 mM 0.0884 mL 0.4419 mL 0.8839 mL 2.2097 mL
    30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8414 mL
    40 mM 0.0552 mL 0.2762 mL 0.5524 mL 1.3811 mL
    50 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1049 mL
    60 mM 0.0368 mL 0.1841 mL 0.3683 mL 0.9207 mL
    80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6905 mL
    100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
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    GSK717 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:

    GSK7171595278-21-9GSK 717GSK-717NOD-like Receptor (NLR)pro-inflammatorycytokinesimmuneresponsesMDP-stimulatedNOD2-TLR2synergyInhibitorinhibitorinhibit

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