2. Apoptosis MAPK/ERK Pathway PI3K/Akt/mTOR Metabolic Enzyme/Protease Autophagy
  3. Apoptosis JNK Akt Caspase FXR Autophagy
  4. Guggulsterone

Guggulsterone  (Synonyms: Z/E-Guggulsterone)

Cat. No.: HY-107738 Purity: 99.78%
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Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.

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

CAS No. : 95975-55-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Guggulsterone:

Guggulsterone Related Antibodies

Top Publications Citing Use of Products

    Guggulsterone purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jan 20:153:157860.  [Abstract]

    Live/dead cell staining using Calcein and PI revealed that Guggulsterone (GS) (10-30 μM; 24 h) induced OS cell death.

    Guggulsterone purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jan 20:153:157860.  [Abstract]

    Guggulsterone (GS) (10-30 μM; 24 h) significantly increased the proportion of apoptotic OS cells.

    Guggulsterone purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jan 20:153:157860.  [Abstract]

    Guggulsterone (GS) (10-30 μM; 24 h) dose-dependently decreased the expression of TOMM20, MFN1, and MFN2 in OS cells.

    Guggulsterone purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2024 Jan-Dec;16(1):2379566.  [Abstract]

    Guggulsterone (E/Z-GS) (10 mg/kg; p.o.; 3 d) reversed the reduction in intestine length, HE scores of inflammation, and ileum damage in NEC (necrotizing enterocolitis) mice.

    Guggulsterone purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2024 Jan-Dec;16(1):2379566.  [Abstract]

    Guggulsterone (E/Z-GS) (10 mg/kg; p.o.; 3 d) reversed the mRNA level of Il6 in the ileum of NEC (necrotizing enterocolitis) mice.

    View All JNK Isoform Specific Products:

    View All Isoforms
    JNK1 JNK2 JNK3 JNK

    View All Akt Isoform Specific Products:

    View All Isoforms
    Akt Akt1 Akt2 Akt3

    View All Caspase Isoform Specific Products:

    View All Isoforms
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1][2]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively[3].

    IC50 & Target[1]

    JNK

     

    Caspase

     

    Cellular Effect
    Cell Line Type Value Description References
    CV-1 IC50
    10 μM
    Compound: Z-Guggulsterone
    Antagonist activity against FXR assessed as transactivation of luciferase reporter gene in CV1 cells
    Antagonist activity against FXR assessed as transactivation of luciferase reporter gene in CV1 cells
    		[PMID: 16905319]
    HEK293 IC50
    12 μM
    Compound: Gs
    Inhibition of FXR in HEK293 cells in presence of CDCA by GAL4 transactivation activity
    Inhibition of FXR in HEK293 cells in presence of CDCA by GAL4 transactivation activity
    		[PMID: 17292610]
    PANC-1 IC50
    42 μM
    Compound: Z-GS
    Cytotoxicity against human PANC1 cells incubated in normal DMEM medium
    Cytotoxicity against human PANC1 cells incubated in normal DMEM medium
    		[PMID: 32057581]
    In Vitro

    Guggulsterone (0.5-20 μM; 24 hours) suppresses TREM-1, TLR4 and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS[2].

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

    Guggulsterone Related Antibodies

    Western Blot Analysis[1]

    Cell Line: RAW 264.7 murine macrophage cells
    Concentration: 0.5, 5, 10, 20 μM
    Incubation Time: 24 hours
    Result: Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.
    In Vivo

    Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis[2].

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

    Animal Model: Wild-type mice with TNBS-induced colitis[2]
    Dosage: 100 mg/kg
    Administration: Orally; once per day; for 8 days
    Result: Improved the survival rates of wild-type mice with TNBS-induced colitis.
    Clinical Trial
    Molecular Weight

    312.45

    Formula

    C21H28O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@]1(/C2=C/C)[C@](CC2=O)([H])[C@@]3([H])[C@]([C@@]4(C(CC3)=CC(CC4)=O)C)([H])CC1
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 20.83 mg/mL (66.67 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 3.2005 mL 16.0026 mL 32.0051 mL
    5 mM 0.6401 mL 3.2005 mL 6.4010 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 (protect from light). 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    90% (20% SBE-β-CD in Saline)

      Solubility: 1.25 mg/mL (4.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.25 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 (12.5 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (4.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (32.01 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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    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: 99.83%

    SDS (393 KB)

    COA (249 KB) HNMR (273 KB) LCMS (277 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 (protect from light). 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 3.2005 mL 16.0026 mL 32.0051 mL 80.0128 mL
    5 mM 0.6401 mL 3.2005 mL 6.4010 mL 16.0026 mL
    10 mM 0.3201 mL 1.6003 mL 3.2005 mL 8.0013 mL
    15 mM 0.2134 mL 1.0668 mL 2.1337 mL 5.3342 mL
    20 mM 0.1600 mL 0.8001 mL 1.6003 mL 4.0006 mL
    25 mM 0.1280 mL 0.6401 mL 1.2802 mL 3.2005 mL
    30 mM 0.1067 mL 0.5334 mL 1.0668 mL 2.6671 mL
    40 mM 0.0800 mL 0.4001 mL 0.8001 mL 2.0003 mL
    50 mM 0.0640 mL 0.3201 mL 0.6401 mL 1.6003 mL
    60 mM 0.0533 mL 0.2667 mL 0.5334 mL 1.3335 mL
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    Guggulsterone 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:

    Guggulsterone95975-55-6Z/E-GuggulsteroneApoptosisJNKAktCaspaseFXRAutophagyc-Jun N-terminal kinasePKBProtein kinase BNR1H4Inhibitorinhibitorinhibit

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