1. Others Metabolic Enzyme/Protease
  2. Oxidative Phosphorylation Proteasome
  3. 4'-Hydroxychalcone

4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.

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4'-Hydroxychalcone Chemical Structure

4'-Hydroxychalcone Chemical Structure

CAS No. : 2657-25-2

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria[1][2][3].

In Vitro

4'-Hydroxychalcone (20-40 μM ; 2 hours) inhibits TNFα-induced (20 ng/mL; 6 hours) NF-kB pathway activation in a dose-dependent manner[3].
4'-Hydroxychalcone (0.1-25 μM ; 8 hours) inhibits proteasome activity in a dose-dependent manner but has no effect on IKK activity[3].
4'-Hydroxychalcone inhibits TNFα-dependent degradation of IkBα and subsequently prevents p50/p65 nuclear translocation leading to 4'-Hydroxychalcone-inhibited expression of NF-kB target genes[3].
4'-Hydroxychalcone affects cancer cell viability but has no significant effect on non-transformed cell viability[3].

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

Cell Viability Assay[3]

Cell Line: K562 cells, Jurkat cells, U937 cells, PBMCs
Concentration: 5 μM, 10 μM, 20 μM, 24 μM, 28 μM, 32 μM, 40 μM, 60 μM
Incubation Time: 24 hours
Result: Affected cancer cell viability but has no significant effect on non-transformed cell viability.

Western Blot Analysis[3]

Cell Line: Jurkat cells
Concentration: 60 μM (followed by TNFα 20 ng/mL )
Incubation Time: 2 hours
Result: Inhibited TNFα -dependent degradation of IkBα and prevents p50/p65 nuclear translocation.
In Vivo

4'-Hydroxychalcone has hepatoprotective activity against Acetaminophen induced hepatotoxicity in mice[2].

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

Animal Model: Male albino mice(5-30 g)[2]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration, 12h intervals, 4 doses
Result: Significantly reduced the mortality rate induced by Acetaminophen (1 g/kg).
Molecular Weight

224.25

Formula

C15H12O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(O)C=C1)/C=C/C2=CC=CC=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 : 250 mg/mL (1114.83 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 4.4593 mL 22.2965 mL 44.5931 mL
5 mM 0.8919 mL 4.4593 mL 8.9186 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)

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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: ≥ 2.08 mg/mL (9.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (9.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

Dosage

mg/kg

Animal weight
(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: 99.66%

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 4.4593 mL 22.2965 mL 44.5931 mL 111.4827 mL
5 mM 0.8919 mL 4.4593 mL 8.9186 mL 22.2965 mL
10 mM 0.4459 mL 2.2297 mL 4.4593 mL 11.1483 mL
15 mM 0.2973 mL 1.4864 mL 2.9729 mL 7.4322 mL
20 mM 0.2230 mL 1.1148 mL 2.2297 mL 5.5741 mL
25 mM 0.1784 mL 0.8919 mL 1.7837 mL 4.4593 mL
30 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7161 mL
40 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7871 mL
50 mM 0.0892 mL 0.4459 mL 0.8919 mL 2.2297 mL
60 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
80 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
100 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
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4'-Hydroxychalcone 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.

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4'-Hydroxychalcone
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