2. Apoptosis Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Metabolic Enzyme/Protease Anti-infection
  3. Apoptosis VEGFR Akt Angiotensin-converting Enzyme (ACE) SARS-CoV FXR
  4. (Z)-Guggulsterone

(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.

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

(Z)-Guggulsterone Chemical Structure

(Z)-Guggulsterone Chemical Structure

CAS No. : 39025-23-5

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of (Z)-Guggulsterone:

(Z)-Guggulsterone Related Antibodies

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(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[1]. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection[2].

IC50 & Target[1]

VEGF-R2

 

Cellular Effect
Cell Line Type Value Description References
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]
In Vitro

(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.

(Z)-Guggulsterone Related Antibodies

Western Blot Analysis[1]

Cell Line: Vascular endothelial growth factor (VEGF)
Concentration: 10, 20 μM
Incubation Time: 24 or 48 hours
Result: Caused a decrease in the level of VEGF-R2 protein in HUVEC.
In Vivo

(Z)-Guggulsterone (oral; 1 mg; 5 times/week) results in a statistically significantly decrease in tumor volume and wet tumor weight[1].

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

Animal Model: Male nude mice (5–6 weeks old) s.c. implanted with DU145 cell-containing Matrigel plugs
Dosage: 1 mg
Administration: Oral; 5 times/week
Result: Resulted in a statistically significantly decrease in tumor volume and wet tumor weight.
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.[Z]
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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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C2

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Volume (final)

V2

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 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.

  • 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

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(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: 99.30%

SDS (393 KB)

COA (249 KB) HNMR (273 KB) LCMS (269 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, 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
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(Z)-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:

(Z)-Guggulsterone39025-23-5ApoptosisVEGFRAktAngiotensin-converting Enzyme (ACE)SARS-CoVFXRVascular endothelial growth factor receptorPKBProtein kinase BSARS coronavirusNR1H4Inhibitorinhibitorinhibit

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