Guggulsterone
Based on 22 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.78%
- No. CAS: 95975-55-6
- Fòrmula: C21H28O2
- Peso molecular:312.45
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Guggulsterone
More- Gut Microbes. 2024 Jan-Dec;16(1):2379566. [Abstract]
- Phytomedicine. 2026 Jan 20:153:157860. [Abstract]
- Phytomedicine. 2025 Aug:144:156949. [Abstract]
- Phytomedicine. 2024 Jul 25:130:155693. [Abstract]
- J Hazard Mater. 2025 Nov 5:499:140149. [Abstract]
- J Ethnopharmacol. 2023 Jan 30:301:115855. [Abstract]
- Ecotoxicol Environ Saf. 2024 Nov 15:287:117266. [Abstract]
- Food Funct. 2026 Jul 6;17(13):6108-6124. [Abstract]
- Nutrients. 2022 Aug 2;14(15):3176. [Abstract]
- Biomolecules. 2025 Jun 28;15(7):943. [Abstract]
- Int Immunopharmacol. 2024 Oct 7;143(Pt 1):113035. [Abstract]
- Int Immunopharmacol. 2023 Oct:123:110768. [Abstract]
- PLoS Pathog. 2022 Jun 13;18(6):e1010620. [Abstract]
- J Inflamm Res. 2025 Mar 4:18:3161-3176. [Abstract]
- Microbiol Spectr. 2022 Oct 26;10(5):e0051822. [Abstract]
- Aquacult Rep. February 2022, 100997.
- Immun Inflamm Dis. 2025 Apr;13(4):e70155. [Abstract]
- Technol Cancer Res Treat. 2023 Jan-Dec:22:15330338231167249. [Abstract]
- Res Sq. 2026 Jan 9.
- bioRxiv. 2025 Nov 8.
- Research Square Preprint. 2023 Oct 28.
- Research Square Preprint. 2020 Dec.
Customer Validation & Images
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Cell Imaging/Staining
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Flow Cytometry
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WB
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Histological Imaging/Staining
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RT-PCR
Ver todos los productos específicos de isoformas Caspase
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Actividad biológica
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JNK |
Caspase |
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Cell Line
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Type | Value | Description | References |
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| CV-1 | IC50 |
10 μM
Compound: Z-Guggulsterone
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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
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[PMID: 16905319] |
| HEK293 | IC50 |
12 μM
Compound: Gs
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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
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[PMID: 17292610] |
| PANC-1 | IC50 |
42 μM
Compound: Z-GS
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Cytotoxicity against human PANC1 cells incubated in normal DMEM medium
Cytotoxicity against human PANC1 cells incubated in normal DMEM medium
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[PMID: 32057581] |
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.
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Cell Line:RAW 264.7 murine macrophage cells
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Concentration:0.5, 5, 10, 20 μM
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Incubation Time:24 hours
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Result:Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type mice with TNBS-induced colitis[2]
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Dosage:100 mg/kg
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Administration:Orally; once per day; for 8 days
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Result:Improved the survival rates of wild-type mice with TNBS-induced colitis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 95975-55-6
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Appearance Solid
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Peso molecular 312.45
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Fòrmula C21H28O2
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Color White to off-white
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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
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Synonyms
Z/E-Guggulsterone
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (22)
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Journal Impact Factor
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Most Recent
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Gut Microbes
Bacteroides fragilis alleviates necrotizing enterocolitis through restoring bile acid metabolism balance using bile salt hydrolase and inhibiting FXR-NLRP3 signaling pathway. [Abstract]2024 Jan-Dec;16(1):2379566. PMID: 39013030
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.
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Phytomedicine
Anti-tumor effects of Guggulsterone in osteosarcoma: Role of SIRT3-mediated PINK1-Parkin mitophagy activation. [Abstract]2026 Jan 20:153:157860. PMID: 41650525
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.
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Phytomedicine
Guggulsterone suppresses osteosarcoma progression by inhibiting glycolysis through MAPK signaling pathway. [Abstract]2025 Aug:144:156949. PMID: 40517691 -
Phytomedicine
Bruceine A alleviates alcoholic liver disease by inhibiting AIM2 inflammasome activation via activating FXR. [Abstract]2024 Jul 25:130:155693. PMID: 38763006 -
J Hazard Mater
Environmental UV filters threaten human neurodevelopment: Disruption of central and peripheral nervous system lineage commitment via WNT signaling dysregulation. [Abstract]2025 Nov 5:499:140149. PMID: 41110322 -
J Ethnopharmacol
Guggulsterone from Commiphora mukul potentiates anti-glioblastoma efficacy of temozolomide in vitro and in vivo via down-regulating EGFR/PI3K/Akt signaling and NF-κB activation. [Abstract]2023 Jan 30:301:115855. PMID: 36280019 -
Ecotoxicol Environ Saf
Aristolochic acid-induced dyslipidemia and hepatotoxicity: The potential role of FXR and AHR receptors. [Abstract]2024 Nov 15:287:117266. PMID: 39509784 -
Food Funct
The hawthorn (Crataegus pinnatifida) procyanidin extract attenuates nonalcoholic fatty liver disease in mice via remodeling the bile acid profile driven by gut microbiota and regulating the FXR pathway. [Abstract]2026 Jul 6;17(13):6108-6124. PMID: 42300918 -
Nutrients
2022 Aug 2;14(15):3176. PMID: 35956351 -
Biomolecules
Significant Reduction of Chenodeoxycholic Acid and Glycochenodeoxycholic Acid in the Elderly with Severe COVID-19. [Abstract]2025 Jun 28;15(7):943. PMID: 40723815 -
Int Immunopharmacol
Novel insights into the role of quercetin and kaempferol from Carthamus tinctorius L. in the management of nonalcoholic fatty liver disease via NR1H4-mediated pathways. [Abstract]2024 Oct 7;143(Pt 1):113035. PMID: 39378656 -
Int Immunopharmacol
Farnesoid X receptor activation is required for the anti-inflammatory and anti-oxidative stress effects of Alisol B 23-acetate in carbon tetrachloride-induced liver fibrosis in mice. [Abstract]2023 Oct:123:110768. PMID: 37573684 -
PLoS Pathog
Bile acids promote the caveolae-associated entry of swine acute diarrhea syndrome coronavirus in porcine intestinal enteroids. [Abstract]2022 Jun 13;18(6):e1010620. PMID: 35696443 -
J Inflamm Res
Saccharomyces boulardii Alleviates Colitis by Regulating FXR-NLRP3 Mediated Macrophage Pyroptosis. [Abstract]2025 Mar 4:18:3161-3176. PMID: 40065908 -
Microbiol Spectr
FXR Signaling-Mediated Bile Acid Metabolism Is Critical for Alleviation of Cholesterol Gallstones by Lactobacillus Strains. [Abstract]2022 Oct 26;10(5):e0051822. PMID: 36036629 -
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Immun Inflamm Dis
Farnesoid X Receptor Regulated Sepsis-Induced Abnormal Bile Acid Metabolism via the Fibroblast Growth Factor 15/Fibroblast Growth Factor Receptor 4 Pathway. [Abstract]2025 Apr;13(4):e70155. PMID: 40192065 -
Technol Cancer Res Treat
DOT1L Epigenetically Regulates Autophagy and Mitochondria Fusion in Cell Lines of Renal Cancer. [Abstract]2023 Jan-Dec:22:15330338231167249. PMID: 37365941 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (32.01 mM); Suspended solution; Need ultrasonic
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- 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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shishodia S, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306. [Content Brief]
[2]. Che X, et al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139. [Content Brief]
[3]. Hsu CW, et al. Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Sci Rep. 2014 Sep 26;4:6437. [Content Brief]
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 |
Guggulsterone Related Classifications
HY-107738 Related Classifications
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