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

Daphnetin (Synonyms: 7,8-Dihydroxycoumarin)

Cat. No.: HY-N0281 Purity: 99.21%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 61 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 55 In-stock
Estimated Time of Arrival: December 31
50 mg USD 209 In-stock
Estimated Time of Arrival: December 31
100 mg USD 385 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Daphnetin

  • Biological Activity

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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)

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].

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].

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.
SMILES

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

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)

H2O : 1 mg/mL (5.61 mM; Need ultrasonic)

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
10 mM 0.5614 mL 2.8068 mL 5.6136 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
References
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Daphnetin
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