Art. -Nr.: HY-N0284

Esculetin

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

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Reinheit: 99.79%
CAS. Nr.: 305-01-1
Formel: C₉H₆O₄
Molecular Weight:178.14

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Esculetin Chemical Structure

CAS. Nr.: 305-01-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3K

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>50 μM Compound: 10; Esc	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 37602711]
HCT-116	IC₅₀	>50 μM Compound: 10; Esc	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 37602711]
Macrophage	IC₅₀	11 μM Compound: 2, aesculetin	Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release by Ellman's method Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release by Ellman's method	[PMID: 8988605]
Macrophage	IC₅₀	11 μmol Compound: 2, aesculetin	Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release by Ellman's method Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release by Ellman's method	[PMID: 8988605]
Macrophage	IC₅₀	18 μM Compound: 2, aesculetin	Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method	[PMID: 8988605]
Macrophage	IC₅₀	18 μmol Compound: 2, aesculetin	Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method	[PMID: 8988605]
MCF7	IC₅₀	>50 μM Compound: 10; Esc	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 37602711]
MCF7	IC₅₀	193 μM Compound: Esculetin	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 38340509]
MDA-MB-231	IC₅₀	>50 μM Compound: 10; Esc	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 37602711]
MDA-MB-231	IC₅₀	7.47 μM Compound: 10; Esc	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs in presence of 3,4-bis(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs in presence of 3,4-bis(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide by MTT assay	[PMID: 37602711]
SK-MEL-28	IC₅₀	0.96 μM Compound: 4	Anticancer activity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Anticancer activity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37197457]
SK-MEL3	IC₅₀	1.7 μM Compound: 4	Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Anticancer activity against human SK-MEL3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37197457]
U-937	CC₅₀	194.1 μM Compound: 2	Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs Cytotoxicity against human U937 cells by trypan blue assay after 48 hrs	[PMID: 18060791]
U-937	IC₅₀	31.33 μM Compound: 2	Growth inhibition of human U937 cells by [3H]thymidine incorporation assay Growth inhibition of human U937 cells by [3H]thymidine incorporation assay	[PMID: 18060791]
U-937	CC₅₀	107.5 μM Compound: 3, Esculetin	Cytotoxicity against human U937 cells after 48 hrs by trypan blue assay Cytotoxicity against human U937 cells after 48 hrs by trypan blue assay	[PMID: 22925447]
U-937	IC₅₀	143.1 μM Compound: 3, Esculetin	Antiproliferative activity against human U937 cells assessed as incorporation of [3H]-methyl-thymidine after 12 hrs by scintillation counting Antiproliferative activity against human U937 cells assessed as incorporation of [3H]-methyl-thymidine after 12 hrs by scintillation counting	[PMID: 22925447]

In Vitro

Esculetin (40 μM, 24 h or 48 h) inhibits PDGF-BB-induced ASMC proliferation and migration^[1].
Esculetin (40 μM, 1 h) inhibits PDGF-BB-induced ECM secretion and activation of PI3K/Akt pathway in ASMC cells^[1].
Esculetin (100 μM, 36 h) induces pancreatic cancer cell (such as PANC-1 cells) apoptosis and loss of mitochondrial membrane potential by activation of caspases 3, 8 and 9^[2].
Esculetin (100 μM, 0-12 h) binds to KEAP1 and inhibits its interaction with Nrf2 in pancreatic cancer cells (in PANC-1 cells)^[2].

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

Western Blot Analysis^[2]

Cell Line:

PANC-1 cells
Concentration:

100 μM
Incubation Time:

0-12 h
Result:

Increased the amount of phosphorylated form of Nrf2.
Increased the levels of Nrf2 in nuclear.
Decreased NF-κB protein levels.

In Vivo

Esculetin (50 and 100 mg/kg/day, p.o., 7d) ameliorates skin lesion in Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice^[3].
Esculetin (10 or 30 mg/kg, i.p., three times per week for 28 days) inhibits tumor growth and metastasis via Axin2 suppression in an HCT116-implanted orthotopic mouse model^[4].
Esculetin (oral gavage, 25 mg/kg for 35 days) inhibits acute restraint stress (ARS)-induced oxidative stress in mature adult mice by increasing antioxidant enzyme activities, the GSH/GSSG ratio, and cytochrome c oxidase activity in cortex^[5].

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

Animal Model:

Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice^[3]
Dosage:

50 and 100 mg/kg/day
Administration:

p.o., 7d
Result:

Ameliorated the skin lesion and reduced the PASI score.
Inhibited epidermal hyperplasia, and CD8 expression in the skin of psoriatic mice.

Chemical Information

CAS. Nr. 305-01-1
Appearance Solid
Molecular Weight 178.14
Formel C₉H₆O₄
Color Yellow to brown
SMILES

O=C1C=CC2=CC(O)=C(O)C=C2O1
Structure Classification
- Phenylpropanoids
- Coumarins
- Phenols
- Polyphenols
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

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Journal Impact Factor

Pharmacol Res

Cardamonin retards progression of autosomal dominant polycystic kidney disease via inhibiting renal cyst growth and interstitial fibrosis. [Abstract]

2020 May;155:104751. PMID: 32151678
Antioxidants (Basel)

Esculetin Improves LPS/D-GalN Induced Acute Liver Injury Through AMPK/SIRT1/PGC-1α Signaling Pathway. [Abstract]

2026 May 21;15(5):652. PMID: 42193273
Chin J Nat Med

2024.
Eur J Pharmacol

BNIP3 as a potential target of esculetin for treating ovarian cancer and prognostic biomarker in ovarian cancer patients. [Abstract]

2025 May 5:177698. PMID: 40334727
Front Cell Dev Biol

Curdione and Schisandrin C Synergistically Reverse Hepatic Fibrosis via Modulating the TGF-β Pathway and Inhibiting Oxidative Stress. [Abstract]

2021 Nov 10;9:763864. PMID: 34858986
J Hepatocell Carcinoma

Inhibitory Effects of Esculetin on Liver Cancer Through Triggering NCOA4 Pathway-Mediation Ferritinophagy in vivo and in vitro. [Abstract]

2023 Apr 11:10:611-629. PMID: 37069958
Toxicol Res

2026 Feb 6.
Folia Histochem Cytobiol

Esculetin ameliorates sevoflurane-induced cognitive dysfunction in aged mice by suppressing neuroinflammation via inhibition of NF-κB/NLRP3 signaling. [Abstract]

2026;64(2):125-139. PMID: 42233475

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (701.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.6136 mL

28.0678 mL

56.1356 mL

5 mM

1.1227 mL

5.6136 mL

11.2271 mL

10 mM

0.5614 mL

2.8068 mL

5.6136 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (11.68 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (11.68 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (11.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xie C, et al. Esculetin regulates the phenotype switching of airway smooth muscle cells. Phytother Res. 2019 Aug 21. [Content Brief]

[2]. Arora R, et al. Esculetin induces antiproliferative and apoptotic response in pancreatic cancer cells by directly binding to KEAP1. Mol Cancer. 2016 Oct 18;15(1):64. [Content Brief]

[3]. Chen Y, et al. Esculetin Ameliorates Psoriasis-Like Skin Disease in Mice by Inducing CD4+Foxp3+ Regulatory T Cells. Front Immunol. 2018 Sep 12;9:2092. [Content Brief]

[4]. Kim WK, et al. Esculetin suppresses tumor growth and metastasis by targeting Axin2/E-cadherin axis in colorectal cancer. Biochem Pharmacol. 2018 Jun;152:71-83. [Content Brief]

[5]. Martín-Aragón S, et al. Age-dependent effects of esculetin on mood-related behavior and cognition from stressed mice are associated with restoring brain antioxidant status. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Feb 4;65:1-16. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	5.6136 mL	28.0678 mL	56.1356 mL	140.3391 mL
	5 mM	1.1227 mL	5.6136 mL	11.2271 mL	28.0678 mL
	10 mM	0.5614 mL	2.8068 mL	5.6136 mL	14.0339 mL
	15 mM	0.3742 mL	1.8712 mL	3.7424 mL	9.3559 mL
	20 mM	0.2807 mL	1.4034 mL	2.8068 mL	7.0170 mL
	25 mM	0.2245 mL	1.1227 mL	2.2454 mL	5.6136 mL
	30 mM	0.1871 mL	0.9356 mL	1.8712 mL	4.6780 mL
	40 mM	0.1403 mL	0.7017 mL	1.4034 mL	3.5085 mL
	50 mM	0.1123 mL	0.5614 mL	1.1227 mL	2.8068 mL
	60 mM	0.0936 mL	0.4678 mL	0.9356 mL	2.3390 mL
	80 mM	0.0702 mL	0.3508 mL	0.7017 mL	1.7542 mL
	100 mM	0.0561 mL	0.2807 mL	0.5614 mL	1.4034 mL

Keywords

Esculetin

8 Cited Publications

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Esculetin

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Publications Citing Use of MedChemExpress (MCE) Esculetin

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit