Cat. No.: HY-N20713

Licocoumarone

Licocoumarone is an active component derived from licorice. Licocoumarone has an IC₅₀ of 12.56 μM and a K_d of 14.90 μM against human DYRK1A. Licocoumarone inhibits NF-κB activation by blocking IκBα degradation and p65 phosphorylation, interferes with MAPK activation via inhibiting phosphorylation, and downregulates the expression of iNOS. Licocoumarone inhibits LPS-induced expression of IL-1β, IL-6 and IL-10; it induces apoptosis of pancreatic cancer cells apoptosis and acts as a neuraminidase inhibitor (IC₅₀ = 27.8 μM). Licocoumarone exhibits anti-inflammatory and antimicrobial activities, with antibacterial activity against Listeria and antifungal activity against Candida parapsilosis. Licocoumarone can be used in studies related to immune and inflammatory diseases, pancreatic cancer, and specific bacterial and fungal infections.

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

CAS No.: 118524-14-4
Formula: C₂₀H₂₀O₅
Molecular Weight:340.37

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Licocoumarone Chemical Structure

CAS No.: 118524-14-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[2]^[1]

DYRK1A

12.56 μM (IC₅₀)

DYRK1A

14.9 μM (Kd)

IL-6

IL-1β

IL-10

iNOS

I-kappaBalpha

All DYRK Isoforms :

All Interleukin Related Isoforms :

All NO Synthase Isoforms :

All NF-κB Isoforms :

All p38 MAPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC₅₀	8.5 μM Compound: 47	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 26841168]
SW480	IC₅₀	5.1 μM Compound: 47	Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay	[PMID: 26841168]

In Vitro

OthersInnate ImmunityCytokines & ChemokinesAnti-cancerApoptosisViral InfectionBacterial InfectionFungal Infection

Others

Licocoumarone (LC) (1.5-100 μM; 24 h) exhibits only extremely low cytotoxicity against RAW 264.7 macrophages even at concentrations as high as 100 μM^[1].
Licocoumarone (compound 5) potently inhibits the enzymatic activity of purified human recombinant DYRK1A, with an IC₅₀ of 12.56 μM and a K_d value of 14.90 μM; it protects purified human recombinant DYRK1A protein from pronase-induced proteolysis^[2].

Innate Immunity

Licocoumarone (1.5-50 μM; 1 h pretreatment followed by 24 h LPS stimulation) dose-dependently inhibits LPS-induced NO production in RAW 264.7 macrophages^[1].
Licocoumarone inhibits LPS-induced NF-κB activation in RAW 264.7 macrophages by reducing the phosphorylation level of p65 and suppressing IκBα degradation; it also inhibits TNF-α-induced NF-κB transcriptional activity in HeLa cells in a dose-dependent manner^[1].
Licocoumarone (3-50 μM; pretreated for 1 hour followed by LPS stimulation for 30 minutes) dose-dependently inhibits LPS-induced phosphorylation of ERK, JNK and p38 MAPKs in RAW 264.7 macrophages^[1].

Cytokines & Chemokines

Innate Immunity

Licocoumarone (3-50 μM; 1 h pretreatment, followed by LPS stimulation for mRNA/24 h for protein) inhibits LPS-induced mRNA and protein expression of iNOS, IL-1β, IL-6 and IL-10 in a dose-dependent manner in RAW 264.7 macrophages, but does not affect the expression of TNF-α^[1].

Anti-cancer

Licocoumarone (0-400 μM; 48 h) potently inhibits the viability of human pancreatic adenocarcinoma BxPC-3 cells, with an IC₅₀ of 50.77 μM after 48 h of treatment^[2].
Licocoumarone (25-50 μM; 2 h) significantly inhibits the proliferation of human pancreatic adenocarcinoma BxPC-3 cells, reducing the proportion of Edu-positive cells to 35.92% and 29.90%, respectively^[2].
Licocoumarone (25-50 μM; initial treatment for 48 h; 7-14 day growth period) significantly reduces the colony-forming ability of human pancreatic adenocarcinoma BxPC-3 cells^[2].
Licocoumarone (50 μM) significantly reduces the expression level of c-MET protein in human pancreatic adenocarcinoma BxPC-3 cells by inhibiting DYRK1A^[2].

Anti-cancer

Apoptosis

Licocoumarone (25-50 μM; 48 h) significantly inhibits the migration of human pancreatic adenocarcinoma BxPC-3 cells; it induces apoptosis in human pancreatic adenocarcinoma BxPC-3 cells, with dose-dependent apoptotic morphological changes (chromatin condensation, nuclear fragmentation) observed^[2].

Viral Infection

Licocoumarone (compound 18) (0.1-1000 μM) reversibly inhibits the neuraminidase in a non-competitive manner, with an IC₅₀ of 27.8 μM and a K_i of 12.1 μM^[3].

Bacterial Infection

Fungal Infection

Licocoumarone (compound 13) selectively inhibits the growth of Bacillus cereus ATCC 11778 and Listeria monocytogenes ATCC 15313 with an MIC of 50 μM; it inhibits Candida parapsilosis ATCC 22019 with an MIC of 100 μM; and at concentrations up to 100 μM, it shows no activity against the tested Gram-negative bacteria, Staphylococcus aureus ATCC 25923, Candida albicans ATCC 10231 or Candida glabrata ATCC 90030^[4].

Bacterial Infection

Licocoumarone (25-50 μM; 24-48 h) exhibits weak, concentration- and biofilm age-dependent activity against preformed Listeria monocytogenes ATCC 15313 biofilms: the maximum eradication rate reaches approximately 45% against 24 h preformed biofilms at 50 μM, while no eradication activity is observed against 48 h preformed biofilms even at the highest concentration of 50 μM^[4].

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

Cell Viability Assay^[1]

Cell Line:

RAW 264.7 mouse macrophages
Concentration:

1.5, 3, 6, 12, 24, 50, 100 μM
Incubation Time:

24 h
Result:

Did not reduce cell viability at concentrations up to 50 μM.
Maintained cell viability at 83.3% at 100 μM, showing minimal cytotoxicity.

Western Blot Analysis^[1]

Cell Line:

LPS-stimulated RAW 264.7 mouse macrophages
Concentration:

3, 12.5, 50 μM
Incubation Time:

1 h pretreatment, followed by 30 min LPS stimulation
Result:

Inhibited LPS-induced phosphorylation of ERK, JNK and p38 in a dose-dependent manner, with the strongest inhibition observed at 50 μM.
Repressed STAT3 phosphorylation solely at 50 μM without detectable activity at lower concentrations.

Real Time qPCR^[1]

Cell Line:

LPS-stimulated RAW 264.7 mouse macrophages
Concentration:

3, 12.5, 50 μM
Incubation Time:

1 h pretreatment, followed by LPS stimulation for mRNA
Result:

Inhibited LPS-induced iNOS, IL-1β, IL-6, and IL-10 mRNA and protein expression in RAW 264.7 macrophages, but does not affect TNF-α expression.

Cell Proliferation Assay^[2]

Cell Line:

human pancreatic adenocarcinoma BxPC-3 cells
Concentration:

25, 50 μM
Incubation Time:

2 h
Result:

Reduced the percentage of Edu-positive proliferating cells from 53.86% to 35.92% and 29.90%, with decreased fluorescent spot number and intensity in treated groups.

Cell Migration Assay ^[2]

Cell Line:

human pancreatic adenocarcinoma BxPC-3 cells
Concentration:

25, 50 μM
Incubation Time:

48 h
Result:

Reduced BxPC-3 cell migration into the denuded zone by approximately twofold and threefold.

Apoptosis Analysis^[2]

Cell Line:

human pancreatic adenocarcinoma BxPC-3 cells
Concentration:

25, 50 μM
Incubation Time:

48 h
Result:

Increased the percentage of apoptotic (Annexin V-FITC/PI positive) cells from 1.10% (control) to 18.50% and 48.60%.

Related Protocols :

Chemical Information

CAS No. 118524-14-4
Molecular Weight 340.37
Formula C₂₀H₂₀O₅
SMILES

OC1=CC(O)=C(C2=CC3=C(C=C(C(C/C=C(C)\C)=C3OC)O)O2)C=C1
Structure Classification
- Phenols
- Polyphenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wu L H, et al. Licocoumarone isolated from Glycyrrhiza uralensis selectively alters LPS-induced inflammatory responses in RAW 264.7 macrophages. European Journal of Pharmacology, 2017, 801: 46-53.

[2]. Zhao C, et al. Licocoumarone induces BxPC-3 pancreatic adenocarcinoma cell death by inhibiting DYRK1A. Chemico-biological interactions. 2020 Jan 25;316:108913. [Content Brief]

[3]. Ryu YB, et al. Inhibition of neuraminidase activity by polyphenol compounds isolated from the roots of Glycyrrhiza uralensis. Bioorganic & medicinal chemistry letters. 2010 Feb 01;20(3):971-4. [Content Brief]

[4]. Çevik D, et al. Evaluation of antimicrobial and antibiofilm activities of secondary metabolites isolated from Glycyrrhiza species. South African Journal of Botany, 2026, 196: 662-673.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Licocoumarone

All DYRK Isoforms

All Interleukin Related Isoforms

All NO Synthase Isoforms

All NF-κB Isoforms

All p38 MAPK Isoforms