1. Metabolic Enzyme/Protease
  2. Fatty Acid Synthase (FASN)
  3. Fatostatin

Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.

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Fatostatin Chemical Structure

Fatostatin Chemical Structure

CAS No. : 125256-00-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Fatostatin:

Top Publications Citing Use of Products
WB
Proliferation Assay

    Fatostatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Oct 28;8(1):431.  [Abstract]

    NUPR1 overexpression‐induced lipogenic enzymes expression can be suppressed by co-incubation with Fatostatin (20 μM; 48 h) in MHCC-97H and SK-Hep1 cells.

    Fatostatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Oct 28;8(1):431.  [Abstract]

    Transwell migration assay. Fatostatin reduces the migration ability of NUPR1-overexpressing MHCC-97H cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 IC50
    10 μM
    Compound: 1, 125B11
    Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis
    Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis
    [PMID: 21561152]
    CHO-K1 IC50
    5.6 μM
    Compound: 1, 125B11
    Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay
    Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay
    [PMID: 21561152]
    In Vitro

    Fatostatin (125B11) (0.1-1 μM; 3 days) inhibits the androgen-independent prostate cancer cell proliferation (IC50=0.1 μM) in an independent of the known IGF1-signaling pathway. Fatostatin inhibits insulin-induced adipogenesis of 3T3-L1 cells[1].
    Fatostatin directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cells.

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

    Cell Proliferation Assay[1]

    Cell Line: DU-145 cells
    Concentration: 0.1, 1 μM
    Incubation Time: 3 days
    Result: Impaired the IGF1-induced growth at an IC50 of 0.1 μM.
    In Vivo

    Fatostatin (125B11) (30 mg/kg; 150 μL; i.p. injection; daily for 28 days) reduces adiposity, ameliorated fatty liver by reducing triglyceride (TG) storage, and lowered hyperglycemia in ob/ob mice[2].

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

    Animal Model: Four-to-five-week-old homozygous male obese (ob/ob) mice (C57BL/6J)[2]
    Dosage: 30 mg/kg; 150 μL
    Administration: i.p. injection; daily for 28 days
    Result: Blocked increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake.
    Molecular Weight

    294.41

    Formula

    C18H18N2S

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CCCC1=NC=CC(C2=NC(C3=CC=C(C)C=C3)=CS2)=C1

    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 : ≥ 27 mg/mL (91.71 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 3.3966 mL 16.9831 mL 33.9662 mL
    5 mM 0.6793 mL 3.3966 mL 6.7932 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
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    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)

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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: ≥ 2.5 mg/mL (8.49 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

      Solubility: 5 mg/mL (16.98 mM); Suspended 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.
    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: 99.96%

    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 3.3966 mL 16.9831 mL 33.9662 mL 84.9156 mL
    5 mM 0.6793 mL 3.3966 mL 6.7932 mL 16.9831 mL
    10 mM 0.3397 mL 1.6983 mL 3.3966 mL 8.4916 mL
    15 mM 0.2264 mL 1.1322 mL 2.2644 mL 5.6610 mL
    20 mM 0.1698 mL 0.8492 mL 1.6983 mL 4.2458 mL
    25 mM 0.1359 mL 0.6793 mL 1.3586 mL 3.3966 mL
    30 mM 0.1132 mL 0.5661 mL 1.1322 mL 2.8305 mL
    40 mM 0.0849 mL 0.4246 mL 0.8492 mL 2.1229 mL
    50 mM 0.0679 mL 0.3397 mL 0.6793 mL 1.6983 mL
    60 mM 0.0566 mL 0.2831 mL 0.5661 mL 1.4153 mL
    80 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0614 mL
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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.

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    Product Name:
    Fatostatin
    Cat. No.:
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