2. 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
  3. EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite
  4. Daphnetin

Daphnetin  (Synonyms: 7,8-Dihydroxycoumarin)

Cat. No.: HY-N0281 Purity: 99.86%
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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-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

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

Daphnetin Chemical Structure

Daphnetin Chemical Structure

CAS No. : 486-35-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 209 In-stock
100 mg USD 385 In-stock
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Based on 2 publication(s) in Google Scholar

Daphnetin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research[1][2][3][4].

IC50 & Target[4]

EGFR

7.67 μM (IC50)

Plasmodium

 

PKA

9.33 μM (IC50)

PKC

25.01 μM (IC50)

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.

Daphnetin Related Antibodies

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.
Molecular Weight

178.14

Formula

C9H6O4
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.6136 mL 28.0678 mL 56.1356 mL
5 mM 1.1227 mL 5.6136 mL 11.2271 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 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.

    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: ≥ 2.5 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.

    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.

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

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: 99.86%

COA (248 KB) HNMR (217 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
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 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
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Daphnetin 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.

Keywords:

Daphnetin486-35-17,8-DihydroxycoumarinEGFRPKAPKCAutophagyApoptosisAMPKAktmTORReactive Oxygen SpeciesCaspaseBcl-2 FamilyPARPParasiteEpidermal growth factor receptorErbB-1HER1Protein kinase AProtein kinase CAMP-activated protein kinasePKBProtein kinase BMammalian target of Rapamycinpoly ADP ribose polymeraseprotein kinaseapoptosisautophagyschizontocidalinflammationA2780 cellsInhibitorinhibitorinhibit

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