1. NF-κB Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation
  2. NF-κB Apoptosis Reactive Oxygen Species
  3. Licochalcone D

Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza uralensis, is a potent and orally active inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties.

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Licochalcone D Chemical Structure

Licochalcone D Chemical Structure

CAS No. : 144506-15-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 319 In-stock
Solution
10 mM * 1 mL in DMSO USD 319 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 290 In-stock
10 mg USD 420 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza uralensis, is a potent and orally active inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties[1][2].

IC50 & Target[1]

p65

 

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
4.85 μM
Compound: 4, LicoD
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production after 18 hrs by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production after 18 hrs by Griess assay
[PMID: 24316124]
In Vitro

Licochalcone D (10 μM; 1 h) negatively regulates Lipopolysaccharides (LPS) (HY-D1056)-induced NF-κB activation by inhibiting the phosphorylation and transactivation of NF-κB p65, inhibits the LPS-induced activation of protein kinase A (PKA), and significantly inhibits the LPS-induced expression of TNFα and MCP-1[1].
Licochalcone D (10 μM; 24 h) significantly inhibits LPS-induced iNOS expression and NO production[1].
Licochalcone D (0-90 μM; 24 h) inhibits the proliferation of human melanoma cells, induces the apoptosis of A375 cells, decreases the mitochondrial membrane potential and increases ROS production in A375 cells[2].
Licochalcone D (0-25 μM; 24 h) decreases the migration and invasion ability of the A375 cells, decreased the protein levels of MMP-2 and MMP-9[2].

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

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 10 μM
Incubation Time: 1 h or 24 h (iNOS), following LPS stimulation (1 μg/mL) for 30 min
Result: Inhibited the phosphorylation of NF-κB at serine 276 but not at serine 536.
Inhibited the LPS-induced expression of TNFα mRNA and MCP-1 mRNA.
Strongly inhibited the expression of iNOS.

Cell Viability Assay[2]

Cell Line: A375 cells or SK-MEL-5
Concentration: 0, 1, 2.5, 5, 15, 30, 45, 60, 75 and 90 μM (A375) or 0, 20, 40, 60 and 80 μM (SK-MEL-5)
Incubation Time: 24 h
Result: Inhibited the proliferation of A375 and SK-MEL-5 in a concentration dependent manner.

Apoptosis Analysis[2]

Cell Line: A375
Concentration: 0, 30, 60 and 90 μM
Incubation Time: 24 h
Result: Cells exhibited obvious apoptotic characteristics after the treatment.

RT-PCR[2]

Cell Line: A375
Concentration: 0, 30, 60 and 90 μM
Incubation Time: 24 h
Result: Downregulated the mRNA level of Bcl-2 and upregulated the mRNA levels of caspase-3, caspase-9 and Bax.

Cell Invasion Assay[2]

Cell Line: A375
Concentration: 25 μM
Incubation Time: 24 h
Result: Significantly suppressed cell invasion.

Cell Migration Assay [2]

Cell Line: A375
Concentration: 25 μM
Incubation Time: 24 h
Result: Significantly suppressed cell migration in the A375 cells.
In Vivo

Licochalcone D (25 and 50 mg/kg; i.g.; daily for a week) inhibits the tumor growth in a mouse xenograft model of murine melanoma B16F0 cells[2].

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

Animal Model: C57BL/6 mice, B16F0 tumor model[2]
Dosage: 25 and 50 mg/kg
Administration: Intragastric administration, daily for a week
Result: Obviously lowered the tumor growth rates, the tumor growth inhibition rates were calculated to be 32.0 and 54.1% at 25 and 50 mg/kg, respectively.
Molecular Weight

354.40

Formula

C21H22O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(O)C(C/C=C(C)\C)=C1)/C=C/C2=CC=C(O)C(O)=C2OC

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (352.71 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 2.8217 mL 14.1084 mL 28.2167 mL
5 mM 0.5643 mL 2.8217 mL 5.6433 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 (protect from light). 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

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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 (5.87 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 (5.87 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:

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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:
%
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+
%
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.81%

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 (protect from light). 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 2.8217 mL 14.1084 mL 28.2167 mL 70.5418 mL
5 mM 0.5643 mL 2.8217 mL 5.6433 mL 14.1084 mL
10 mM 0.2822 mL 1.4108 mL 2.8217 mL 7.0542 mL
15 mM 0.1881 mL 0.9406 mL 1.8811 mL 4.7028 mL
20 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5271 mL
25 mM 0.1129 mL 0.5643 mL 1.1287 mL 2.8217 mL
30 mM 0.0941 mL 0.4703 mL 0.9406 mL 2.3514 mL
40 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
50 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
60 mM 0.0470 mL 0.2351 mL 0.4703 mL 1.1757 mL
80 mM 0.0353 mL 0.1764 mL 0.3527 mL 0.8818 mL
100 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
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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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Licochalcone D
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