JAK/STAT Signaling Protein Tyrosine Kinase/RTK TGF-beta/Smad Stem Cell/Wnt Epigenetics Autophagy Apoptosis PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage Anti-infection
EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species (ROS) Caspase Bcl-2 Family PARP Parasite
Daphnetin

Referencia número: HY-N0281

Daphnetin

(Synonyms: 7,8-Dihydroxycoumarin)

7 Cited Publications

Revisión del cliente

Based on 7 publication(s) in Google Scholar

Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

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Pureza: 99.77%
No. CAS: 486-35-1
Fòrmula: C₉H₆O₄
Peso molecular:178.14

Almacenamiento:

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

Daphnetin Chemical Structure

No. CAS: 486-35-1

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (7)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[4]

EGFR

7.67 μM (IC₅₀)

Plasmodium

PKA

9.33 μM (IC₅₀)

PKC

25.01 μM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

Ver todos los productos específicos de isoformas PKA :

Ver todos los productos específicos de isoformas PKC :

Ver todos los productos específicos de isoformas AMPK :

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Ver todos los productos específicos de isoformas PARP :

Ver todos los productos específicos de isoformas Parasite :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	73 μM Compound: Daphnetin	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]
U-937	CC₅₀	120.2 μM Compound: 20	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs	[PMID: 26188907]
U-937	IC₅₀	83.2 μM Compound: 20	Antiproliferative activity against human U937 cells after 3 days Antiproliferative activity against human U937 cells after 3 days	[PMID: 26188907]

In Vitro

Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells^[1].
Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner^[1].
Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway^[1].
Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner^[3].

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

Cell Viability Assay^[1]

Cell Line:

IOSE8C, A2780, SKOV3 and OVCAR8 cells
Concentration:

0, 5, 10, 20 and 40 µg/mL
Incubation Time:

24 h and 48 hours
Result:

Inhibited growth in ovarian cancer cells but not in normal cells.

Apoptosis Analysis^[1]

Cell Line:

A2780 and SKOV3 cells
Concentration:

0, 10, 20 and 40 µg/mL
Incubation Time:

24 hours
Result:

Increased apoptosis in a dose-dependent manner in A2780 and SKOV3 cells.

Western Blot Analysis^[1]

Cell Line:

A2780 and SKOV3 cells
Concentration:

0, 10, 20 and 40 µg/mL
Incubation Time:

24 hours
Result:

Increased proapoptotic protein (Caspase 3, Bax, and PARP) expression but decreased antiapoptotic protein (Bcl2) expression.

Western Blot Analysis^[1]

Cell Line:

A2780 cells
Concentration:

0, 10, 20 and 40 µg/mL
Incubation Time:

24 hours
Result:

Increased LC3 II and p62 expression in a dose-dependent manner and reduced the expression levels of p-Akt, p-mTOR, but increased the expression level of p-AMPK.

In Vivo

Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model^[1].
Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1^[2].
Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo^[3].

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

Animal Model:

BALB/c nude mice^[1]
Dosage:

30 mg/kg
Administration:

Intraperitoneal injection; Daily; for 12 days
Result:

Decreased tumor volume and weight in a xenograft animal model.

Animal Model:

Male Kunming outbred strain mice^[3]
Dosage:

10, 50 or 100 mg/kg
Administration:

Oral gavage and intraperitoneal injection; every four days, for 30 days
Result:

Reduced the number of parasites in mice.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 486-35-1
Appearance Solid
Peso molecular 178.14
Fòrmula C₉H₆O₄
Color Off-white to yellow
SMILES

O=C1C=CC2=CC=C(O)C(O)=C2O1
Synonyms

7,8-Dihydroxycoumarin
Structure Classification
- Phenylpropanoids
- Coumarins
- Phenols
- Polyphenols
Initial Source
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (7)

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Journal Impact Factor

Int Immunopharmacol

Daphnetin alleviates silica-induced pulmonary inflammation and fibrosis by regulating the PI3K/AKT1 signaling pathway in mice. [Abstract]

2024 May 30:133:112004. PMID: 38613881
Biol Res

Daphnetin alleviates unexplained recurrent spontaneous abortion by regulating the NR4A1/BACH2 axis in mice. [Abstract]

2025 Dec 29;58(1):77. PMID: 41462398
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
J Cell Commun Signal

Daphnetin alleviates inflammation and promotes autophagy via the AMPK/mTOR pathway in gouty arthritis. [Abstract]

2025 Apr 28;19(2):e70011. PMID: 40304008
Am J Pathol

α-Subunit Tyrosine Phosphorylation Is Required for Activation of the Large Conductance Ca2+-Activated Potassium Channel in the Rabbit Sphincter of Oddi. [Abstract]

2022 Dec;192(12):1725-1744. PMID: 36150507
Pharmacology

Daphnetin Preconditioning Decreases Cardiac Injury and Susceptibility to Ventricular Arrhythmia following Ischaemia-Reperfusion through the TLR4/MyD88/NF-Κb Signalling Pathway. [Abstract]

2021;106(7-8):369-383. PMID: 33902056
Histol Histopathol

Daphnetin alleviates renal inflammation, oxidative stress, and apoptosis in septic rats via the JAK2/STAT3 signaling pathway. [Abstract]

2025 Sep 3:18978. PMID: 40899121

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (280.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (14.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (14.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (14.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 25 mg/mL (140.34 mM); Suspended solution; Need ultrasonic

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Fan X, et, al. Daphnetin triggers ROS-induced cell death and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway in ovarian cancer. Phytomedicine. 2021 Feb;82:153465. [Content Brief]

[2]. Zhang L, et, al. Daphnetin protects against cisplatin-induced nephrotoxicity by inhibiting inflammatory and oxidative response. Int Immunopharmacol. 2018 Dec;65:402-407. [Content Brief]

[3]. Wang QM, et, al. The schizontocidal activity of daphnetin against malaria parasites in vitro and in vivo. Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 2000;18(4):204-6. [Content Brief]

[4]. Yang EB, Zhao YN, Zhang K, Mack P. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem Biophys Res Commun. 1999 Jul 14;260(3):682-5. [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

Daphnetin

7 Cited Publications

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Daphnetin

Anti-Infection Compound Library

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