Art. -Nr.: HY-107738

Guggulsterone

(Synonyms: Z/E-Guggulsterone)

22 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.78%
CAS. Nr.: 95975-55-6
Formel: C₂₁H₂₈O₂
Molecular Weight:312.45

Speicherung:

4°C, protect from light

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

Guggulsterone Chemical Structure

CAS. Nr.: 95975-55-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 95975-55-6
Appearance Solid
Molecular Weight 312.45
Formel C₂₁H₂₈O₂
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
Synonyms

Z/E-Guggulsterone
Structure Classification
- Terpenoids
- Triterpenes
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (22)

All Histological Imaging/StainingCell Imaging/StainingRT-PCRFlow CytometryWB

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Journal Impact Factor

J Hazard Mater

Environmental UV filters threaten human neurodevelopment: Disruption of central and peripheral nervous system lineage commitment via WNT signaling dysregulation. [Abstract]

2025 Oct 17:499:140149. PMID: 41110322
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.
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.
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
Ecotoxicol Environ Saf

Aristolochic acid-induced dyslipidemia and hepatotoxicity: The potential role of FXR and AHR receptors. [Abstract]

2024 Nov 5:287:117266. 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
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
Nutrients

Glycochenodeoxycholate Affects Iron Homeostasis via Up-Regulating Hepcidin Expression. [Abstract]

2022 Aug 2;14(15):3176. PMID: 35956351
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
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
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
Aquacult Rep

February 2022, 100997.
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
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
Res Sq

2026 Jan 9.
bioRxiv

2025 Nov 8.
Research Square Preprint

2023 Oct 28.
Research Square Preprint

2020 Dec.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2005 mL

16.0026 mL

32.0051 mL

5 mM

0.6401 mL

3.2005 mL

6.4010 mL

10 mM

0.3201 mL

1.6003 mL

3.2005 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Guggulsterone

22 Cited Publications

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Guggulsterone

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Publications Citing Use of MedChemExpress (MCE) Guggulsterone

Alle JNK Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit