2. NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Keap1-Nrf2 Glutathione Peroxidase Ferroptosis
  4. Gingerenone A

Gingerenone A is an Nrf2-Gpx4 activator that can induce Ferroptosis in liver damage with oral activity. Gingerenone A has anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging effects in mice.

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Gingerenone A Chemical Structure

Gingerenone A Chemical Structure

CAS No. : 128700-97-0

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Based on 1 publication(s) in Google Scholar

Gingerenone A Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Gingerenone A is an Nrf2-Gpx4 activator that can induce Ferroptosis in liver damage with oral activity. Gingerenone A has anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging effects in mice[1][2][3][4].

IC50 & Target

Nrf2-Gpx4[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
24 μM
Compound: 40
Cytotoxicity against HEK293 cells after 16 hrs by alamar blue assay
Cytotoxicity against HEK293 cells after 16 hrs by alamar blue assay
[PMID: 20004045]
In Vitro

Gingerenone A (2.5-40 μM, 5 h) overcomes insulin resistance and increases glucose uptake in 3T3-L1 cells by inhibiting S6K1 activity[1].
Gingerenone A (40 μM, 6 days) inhibits lipogenesis and lipid accumulation in 3T3-L1 cells[2].
Gingerenone A (0-40 μM, 6 days) suppresses the proliferation and hypertrophy of 3T3-L1 cells, regulating the expression or phosphorylation levels of proteins related to lipogenesis and fatty acid metabolism[2].
Gingerenone A promotes anti-proliferation and senescence in breast cancer cells induced by oxidative stress[3].
Gingerenone A with an IC50 values for breast cancer cells (SKBR3, MCF-7 and MDA-MB-231) is 50.41, 42.67, 56.29 µM in a 48-hour TP experiment [3].
Gingerenone A (80 μM, 48 h) causes a delay in the G2/M phase of MCF7 and MDA-MB-231 cells[3].
Gingerenone A (80 μM, 1.5-3 h) induces an increase in ROS levels in MCF7 and MDA-MB-231 cells[3].
Gingerenone A (0-80 μM, 48 h) induces senescence in MCF7 and MDA-MB-231 cells[3].

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

Gingerenone A Related Antibodies

Western Blot Analysis[1]

Cell Line: 3T3-L1
Concentration: 0, 2.5, 5, 10, 20, 40 μM
Incubation Time: 5 h
Result: Increased AKTS473 and S6K1T389, decreased phosphorylation of S6S235/236 and insulin receptor substrate 1 (IRS-1) S1101, and increased binding of IRS-1 to PI3K.

Immunofluorescence[2]

Cell Line: 3T3-L1
Concentration: 40 μM
Incubation Time: 6 days
Result: Inhibits cellular adipogenesis and lipid accumulation.

Western Blot Analysis[2]

Cell Line: 3T3-L1
Concentration: 0, 10, 20, 40 μM
Incubation Time: 6 days
Result: Inhibited PPAR-γ, C/EBP-α, and FAS protein levels, decreased SREBP-1 and FAS (lipogenesis markers) protein expression levels, and increased PGC-1α and CPT-1 (fatty acid oxidation markers) protein expression levels.

Cell Viability Assay[3]

Cell Line: MCF7, SKBR3, M10, MDA-MB-231
Concentration: 0, 20, 40, 60, 80μM
Incubation Time: 48 h
Result: Inhibited tumor cell proliferation with little effect on normal cells.

Cell Cycle Analysis[3]

Cell Line: MCF7, MDA-MB-231
Concentration: 80 μM
Incubation Time: 48 h
Result: Increased subG1, moderately decreased G1, and increased G2/M populations.

Real Time qPCR[3]

Cell Line: MCF-7, MDA-MB-231
Concentration: 0, 40, 80 μM
Incubation Time: 5 h
Result: Upregulated the expression of aging-related genes EDN1, ANKRD1, CDKN1A, SERPINE and TAGLN.
In Vivo

Gingerenone A (10-50 mg/kg, orally, once a day, 15 weeks) reduces the increase in fat mass induced by a high-fat diet in mice by decreasing the size of fat cells, thereby inhibiting obesity and inflammation in adipose tissue[2].
Gingerenone A (5-20 mg/kg, orally, once a day, 7 days) can alleviate ferroptosis in the SLI of DSS-induced colitis mice, and its protective effect is associated with the activation of the Nrf2-Gpx4 signaling pathway[4].

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

Animal Model: HFD mice[2]
Dosage: 10, 50 mg/kg; daily; 15 weeks
Administration: Oral
Result: Reduced fat gain without significantly affecting caloric intake, reduced visceral fat mass, and made fat cells smaller.
Animal Model: Mice induced by DSS[6]
Dosage: 5, 20 mg/kg; daily; 7 days
Administration: Oral
Result: Alleviated DSS-induced liver pathological damage, liver parameters and cytokine levels, increased antioxidant enzyme activities, alleviated ferroptosis, upregulated GPX4 expression, and activated Nrf2.
Molecular Weight

356.41

Formula

C21H24O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(/C=C/CCC1=CC=C(O)C(OC)=C1)CCC2=CC=C(O)C(OC)=C2
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 : 100 mg/mL (280.58 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 2.8058 mL 14.0288 mL 28.0576 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 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)

Mass
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Volume
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Molecular Weight *

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.01 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.01 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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
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 2.8058 mL 14.0288 mL 28.0576 mL 70.1439 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 mL 14.0288 mL
10 mM 0.2806 mL 1.4029 mL 2.8058 mL 7.0144 mL
15 mM 0.1871 mL 0.9353 mL 1.8705 mL 4.6763 mL
20 mM 0.1403 mL 0.7014 mL 1.4029 mL 3.5072 mL
25 mM 0.1122 mL 0.5612 mL 1.1223 mL 2.8058 mL
30 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7536 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4029 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
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Gingerenone A 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:

Gingerenone A128700-97-0Keap1-Nrf2Glutathione PeroxidaseFerroptosisAnti-inflammatoryanti-diabeticanti-tumorpro-agingInhibitorinhibitorinhibit

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