(Z)-Guggulsterone
Based on 6 publication(s) in Google Scholar
(Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection.
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- Purity: 99.41%
- CAS No.: 39025-23-5
- 화학식: C21H28O2
- 분자량:312.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) (Z)-Guggulsterone
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Cell Migration/Invasion Assay
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WB
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IF
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
All VEGFR Isoforms
More
Biological Activity
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VEGF-R2 |
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Cell Line
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Type | Value | Description | References |
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| 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] |
(Z)-Guggulsterone (10, 20 μM; 24 or 48 hours) causes a decrease in the level of VEGF-R2 protein in HUVEC[1].
(Z)-Guggulsterone (10 μM; 24 h) reduces ACE2 and SHP levels in primary airway and intestinal organoids, and reduces SARS-CoV-2 infection in multiple cell types via FXR-mediated ACE2 regulation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vascular endothelial growth factor (VEGF)
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Concentration:10, 20 μM
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Incubation Time:24 or 48 hours
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Result:Caused a decrease in the level of VEGF-R2 protein in HUVEC.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude mice (5–6 weeks old) s.c. implanted with DU145 cell-containing Matrigel plugs
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Dosage:1 mg
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Administration:Oral; 5 times/week
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Result:Resulted in a statistically significantly decrease in tumor volume and wet tumor weight.
Chemical Information
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CAS No. 39025-23-5
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Appearance Solid
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분자량 312.45
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화학식 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.[Z]
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Bone Res
Nuclear farnesoid X receptor protects against bone loss by driving osteoblast differentiation through stabilizing RUNX2. [Abstract]2025 Jan 30;13(1):20. PMID: 39885145 -
Research (Wash D C)
Activation of Pancreatic Acinar FXR Protects against Pancreatitis via Osgin1-Mediated Restoration of Efficient Autophagy. [Abstract]2022 Nov 2:2022:9784081. PMID: 36405253 -
Pharmacol Res
Lactobacillus rhamnosus GG ameliorates triptolide-induced liver injury through modulation of the bile acid-FXR axis. [Abstract]2024 Jun 20:107275. PMID: 38908615 -
Cell Death Dis
FXR deficiency induced ferroptosis via modulation of the CBP-dependent p53 acetylation to suppress breast cancer growth and metastasis. [Abstract]2024 Nov 14;15(11):826. PMID: 39543094
(Z)-Guggulsterone purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 14;15(11):826. [Abstract]
(Z)-Guggulsterone (Z-GS) (20, 40 μM) treatment significantly reduced the invasion abilities of breast cancer cells pretreated with TGF-β1.
(Z)-Guggulsterone purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 14;15(11):826. [Abstract]
The proteins levels of E-Cadherin, N-Cadherin, and vimentin in MDA-MB-231 cells were measured by western blotting assays treated with (Z)-Guggulsterone (Z-GS) (20, 40 μM).
(Z)-Guggulsterone purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 14;15(11):826. [Abstract]
The relative levels of lipid ROS were detected by the C11-BODIPY probe in MDA-MB-231 cells treated with (Z)-Guggulsterone (Z-GS) (20, 40 μM).
(Z)-Guggulsterone purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 14;15(11):826. [Abstract]
The viability of MDA-MB-231 cells cultured with (Z)-Guggulsterone (Z-GS) (20, 40 μM) in the presence or absence of various cell death inhibitors was detected by CCK8.
(Z)-Guggulsterone purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 14;15(11):826. [Abstract]
Tumor metastasis was determined by H&E staining assay treated with (Z)-Guggulsterone (Z-GS) (30 mg/kg, i.p.).
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Int J Biol Macromol
Salidroside attenuates NASH through regulating bile acid-FXR/TGR5 signaling pathway via targeting gut microbiota. [Abstract]2025 Mar 19:142276. PMID: 40118401 -
용액&용해도
DMSO : 10 mg/mL (32.01 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
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.
순도&문서
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Data Sheet (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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Xiao D, et al. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80. [Content Brief]
[2]. Brevini T, et al. FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2. Nature. 2022 Dec 5. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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 |