2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  3. PPAR Apoptosis
  4. GW6471

GW6471 is a selective peroxisome proliferator-activated receptor α (PPARα) antagonist. GW6471 reduces cancer stem cell viability, proliferation, and spheroid formation. GW6471 induces apoptosis and causes metabolic impairment including energy imbalance. GW6471 can be used for the research of paragangliomas and triple-negative breast cancer.

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

CAS No. : 880635-03-0

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Customer Review

Based on 70 publication(s) in Google Scholar

GW6471 Related Antibodies

Top Publications Citing Use of Products

70 Publications Citing Use of MCE GW6471

IF
RT-PCR
WB

    GW6471 purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2023 Apr;106(4):2271-2288.  [Abstract]

    GW6471 significantly reduces the regulatory effects of GINY and DQW on the protein expression levels of PPARα, CPT-1a, ACOX1, HO-1, and FASN in HepG2 cells.

    GW6471 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803.  [Abstract]

    Cells are treated with PE (50 μM), zileuton (100 μM), and GW6471 (10 μM) for 24 h. α-Actinin staining (n = 6) results in H9c2 cells.

    GW6471 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803.  [Abstract]

    The antihypertrophic effects of zileuton ar counteracted by GW6471 as indicated by increased PE-induced hypertrophic marker transcription, cell surface area, and oxidative stress when compared with those in the PE group and PE+ zileuton group.

    View All PPAR Isoform Specific Products:

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    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW6471 is a selective peroxisome proliferator-activated receptor α (PPARα) antagonist. GW6471 reduces cancer stem cell viability, proliferation, and spheroid formation. GW6471 induces apoptosis and causes metabolic impairment including energy imbalance. GW6471 can be used for the research of paragangliomas and triple-negative breast cancer[1][2][3].

    IC50 & Target[1]

    PPARα

     

    In Vitro

    GW6471 (7-16 μM; 72 h) reduces cell viability in PTJ64i and PTJ86i head and neck paraganglioma cell lines at 16 μM[1].
    GW6471 (7-16 μM; 72 h) impairs clonogenicity in PTJ64i and PTJ86i head and neck paraganglioma cell lines, with 16 μM causing a more drastic reduction in colony-forming capacity than 7 μM[1].
    GW6471 (4-16 μM; 72 h) dose-dependently reduces cell viability in MDA-MB-231-derived breast cancer stem cell mammospheres, with significant effects observed at 4 μM, 8 μM, and 16 μM after 72 hours of treatment[3].
    GW6471 (8 μM; 72 h) induces significant cytotoxicity in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) significantly inhibits spheroid growth in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) induces G1 phase cell cycle arrest and intrinsic pathway apoptosis in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) activates caspase 3/7, confirming apoptotic induction in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) activates p-AMPK, reduces lipid droplet and cholesterol levels, and downregulates mevalonate pathway gene expression in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) impairs glucose metabolism in MDA-MB-231-derived breast cancer stem cell mammospheres by downregulating key glycolytic proteins, reducing glucose uptake, and decreasing lactate production[3].
    GW6471 (8 μM; 72 h) upregulates CD36 and induces nuclear translocation of PPARγ in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) activates GSK3β and reduces cytoplasmic/nuclear β-catenin while increasing membrane-associated β-catenin in MDA-MB-231-derived breast cancer stem cell mammospheres[3].
    GW6471 (8 μM; 72 h) reduces YAP/TAZ activity, downregulates Rho family proteins, and inhibits invasion in MDA-MB-231-derived breast cancer stem cell mammospheres[3].

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

    GW6471 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: PTJ64i, PTJ86i (head and neck paraganglioma cell lines)
    Concentration: 7 μM; 16 μM
    Incubation Time: 72 h
    Result: Reduced cell viability in PTJ64i and PTJ86i head and neck paraganglioma cell lines at 16 μM.
    Impaired clonogenicity in PTJ64i and PTJ86i head and neck paraganglioma cell lines, with 16 μM causing a more drastic reduction in colony-forming capacity than 7 μM

    Cell Viability Assay[3]

    Cell Line: MDA-MB-231-derived breast cancer stem cell mammospheres
    Concentration: 4 μM; 8 μM; 16 μM
    Incubation Time: 72 h
    Result: Reduced cell viability to ~70% of control at 4 μM.
    Reduced cell viability to ~40% of control at 8 μM.
    Reduced cell viability to ~25% of control at 16 μM.

    Cell Cytotoxicity Assay[3]

    Cell Line: MDA-MB-231-derived breast cancer stem cell mammospheres
    Concentration: 8 μM
    Incubation Time: 72 h
    Result: Increased mean fluorescence intensity (cytotoxicity) in a time-dependent manner over 72 hours.
    Showed significantly higher cytotoxicity levels compared to untreated controls at all time points after 0 hours.

    Cell Cycle Analysis[3]

    Cell Line: MDA-MB-231-derived breast cancer stem cell mammospheres
    Concentration: 8 μM
    Incubation Time: 72 h
    Result: Induced G1 phase cell cycle arrest and intrinsic pathway apoptosis.

    Apoptosis Analysis[3]

    Cell Line: MDA-MB-231-derived breast cancer stem cell mammospheres
    Concentration: 8 μM
    Incubation Time: 72 h
    Result: Increased mean fluorescence intensity indicating caspase 3/7 activation over the 72-hour period.
    Molecular Weight

    619.67

    Formula

    C35H36F3N3O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    CCC(NC[C@@H](N/C(C)=C\C(C1=CC=C(C(F)(F)F)C=C1)=O)CC2=CC=C(OCCC3=C(C)OC(C4=CC=CC=C4)=N3)C=C2)=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 : 83.33 mg/mL (134.47 mM; ultrasonic and warming and heat to 60°C; 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 1.6138 mL 8.0688 mL 16.1376 mL
    5 mM 0.3228 mL 1.6138 mL 3.2275 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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    In Vivo:

    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:  15% Cremophor EL    85% Saline

      Solubility: 5.56 mg/mL (8.97 mM); Suspended solution; Need ultrasonic

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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.64%

    SDS (393 KB)

    COA (247 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 1.6138 mL 8.0688 mL 16.1376 mL 40.3441 mL
    5 mM 0.3228 mL 1.6138 mL 3.2275 mL 8.0688 mL
    10 mM 0.1614 mL 0.8069 mL 1.6138 mL 4.0344 mL
    15 mM 0.1076 mL 0.5379 mL 1.0758 mL 2.6896 mL
    20 mM 0.0807 mL 0.4034 mL 0.8069 mL 2.0172 mL
    25 mM 0.0646 mL 0.3228 mL 0.6455 mL 1.6138 mL
    30 mM 0.0538 mL 0.2690 mL 0.5379 mL 1.3448 mL
    40 mM 0.0403 mL 0.2017 mL 0.4034 mL 1.0086 mL
    50 mM 0.0323 mL 0.1614 mL 0.3228 mL 0.8069 mL
    60 mM 0.0269 mL 0.1345 mL 0.2690 mL 0.6724 mL
    80 mM 0.0202 mL 0.1009 mL 0.2017 mL 0.5043 mL
    100 mM 0.0161 mL 0.0807 mL 0.1614 mL 0.4034 mL
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    GW6471 Related Classifications

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    • 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:

    GW6471880635-03-0GW 6471GW-6471PPARApoptosisPeroxisome proliferator-activated receptorsPTJ86iMDA-MB-231cardiomyocytemurine embryonic stem cellscancer stem cellhead and neck paraganglioma cellsPTJ64iperoxisome proliferator-activated receptor αtriple-negative breast cancerPPARαInhibitorinhibitorinhibit

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