2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. GSK0660

GSK0660 is a potent PPARβ antagonist with an IC50 of 155 nM.

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

CAS No. : 1014691-61-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
250 mg In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of GSK0660:

GSK0660 Related Antibodies

Top Publications Citing Use of Products

    GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212.  [Abstract]

    Cell proliferation quantified using EdU uptake (left) and FACS analysis of the cell cycle progression (right) in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) malignant human keratinocytes (SCC13).

    GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212.  [Abstract]

    Expression of p21 at mRNA (CDKA1A, quantified by qPCR; left) and protein (representative western blot, middle panel; right panel represents the quantification of three independent western blots) in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.

    GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212.  [Abstract]

    Representative western blots (left) of three independent western blots (right) of phosphorylated H2AX (γH2AX) (upper panel), of total and phosphorylated CHK1 (middle panels), and of p21 at 0, 0.5, 2, and 6 h after UVB‐exposure in control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.

    GSK0660 purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Dec 15;38(23):e70212.  [Abstract]

    Percentage of apoptotic cells in response to UVB exposure using FACS analysis of Annexin V on control (DMSO) and PPARβ‐inhibited (GSK0660) (5 μM) SCC13 cells.

    View All PPAR Isoform Specific Products:

    View All Isoforms
    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK0660 is a potent PPARβ antagonist with an IC50 of 155 nM.

    IC50 & Target[1]

    PPARβ/δ

    155 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    C2C12 IC50
    48 nM
    Compound: GSK0660
    Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis
    Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis
    		[PMID: 22369181]
    In Vitro

    GSK0660 is a potent antagonist of PPARβ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both >10 μM. GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.8. GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells[1].
    GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells. GSK0660 (0.1 and 0.5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells[2].
    GSK0660 (1 μM) markedly blocks GW501516-mediated attenuation of glutamate release, and the effect of GW501516 on ROS generation in BV-2 cells stimulated with LPS. Furthermore, GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells[3].

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

    GSK0660 Related Antibodies
    Molecular Weight

    418.49

    Formula

    C19H18N2O5S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC
    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 : ≥ 49 mg/mL (117.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3895 mL 11.9477 mL 23.8954 mL
    5 mM 0.4779 mL 2.3895 mL 4.7791 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.5 mg/mL (5.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

    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.
    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
    References
    Cell Assay
    [2]

    Cell viability is determined by the MTT dye. MC3T3-E1 cells are incubated with bezafibrate (1−1000 μM) for 24, 48, or 72 h, and are pretreated with the AMPK inhibitor compound C (5 μM), PPARβ inhibitor GSK0660 (0.5 μM), PPARα inhibitor MK886 (10 μM), or NOS inhibitor L-NAME (1000 μM) followed by bezafibrate (100 μM) incubation for 48 h. After the incubations, 10 μL of MTT is added to each well of a 96-well microplate, and the microplates are placed in an incubator at 37°C for 4 h. One hundred fifty microliters of DMSO is added to all wells and mixed thoroughly to lyse the cells and dissolve the dark blue crystals. After 10 min, the absorbance is measured at 570 nm using a microplate reader[2].

    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, 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 2.3895 mL 11.9477 mL 23.8954 mL 59.7386 mL
    5 mM 0.4779 mL 2.3895 mL 4.7791 mL 11.9477 mL
    10 mM 0.2390 mL 1.1948 mL 2.3895 mL 5.9739 mL
    15 mM 0.1593 mL 0.7965 mL 1.5930 mL 3.9826 mL
    20 mM 0.1195 mL 0.5974 mL 1.1948 mL 2.9869 mL
    25 mM 0.0956 mL 0.4779 mL 0.9558 mL 2.3895 mL
    30 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
    40 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4935 mL
    50 mM 0.0478 mL 0.2390 mL 0.4779 mL 1.1948 mL
    60 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9956 mL
    80 mM 0.0299 mL 0.1493 mL 0.2987 mL 0.7467 mL
    100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5974 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    GSK0660 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:

    GSK06601014691-61-2GSK 0660GSK-0660PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GSK0660
    Cat. No.:
    HY-12377
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.