Daphnetin

SKU: orb1304931

Description

Daphnetin (7,8-Dihydroxycoumarin) is a natural protein kinase inhibitor targeting EGFR, PKA, and PKC. It also possesses antioxidant and anti-inflammatory properties, supporting its investigation in cellular assays and animal models for oncology and inflammatory disease research.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation, Infectious Disease & Virology, Metabolism Research, Molecular Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 486-35-1
• MW: 178.14
• Purity: 99.82% (May vary between batches)
• Formula: C₉H₆O₄
• SMILES: Oc1ccc2ccc(=O)oc2c1O
• Target: Autophagy,PKA,Akt,Bcl-2 Family,mTOR,Reactive Oxygen Species,EGFR,PARP,AMPK,PKC,Parasite,ROS,Apoptosis,Caspase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (11.23 mM);DMSO:50 mg/mL (280.68 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR:7.67 μM|PKC:25.01 μM|PKA:9.33 μM
• In Vivo:
  Daphnetin, at concentrations between 25-40 μM, achieves a 50% inhibition rate against the incorporation of hypoxanthine induced by malignant malaria parasites. At a higher concentration of 50 μM, Daphnetin significantly reduces the levels of cyclin D1. It counteracts the reduction in cell viability caused by dexamethasone, which affects cortical neurons, in a dose-dependent manner. Daphnetin also inhibits the activity of endogenous or recombinant TaPRK in a specific, dose-dependent way. Moreover, it effectively inhibits tyrosine phosphorylation of exogenous substrates catalyzed by the epidermal growth factor receptor, in addition to inhibiting the activity of PKA and PKC. Treatment with Daphnetin for 24 hours suppresses the growth of the human cancer cell line MCF-7, which responds to estrogen (IC50: 73 μM), and inhibits the ERK1/ERK2 mitogenic signaling pathway.
• In Vitro:
  In water maze and forced swimming tests, Daphnetin (2-8 mg/kg) significantly improved the performance of stressed mice. At a dosage of 140 mg/kg, Daphnetin was able to reduce uterine weight by 39.5%. Additionally, Daphnetin markedly prolonged the survival time of mice infected with P. yoelii.
• Cell Research:
  The cytostatic effect of Daphnetin tested on the MCF-7 tumor cells is estimated using the microculture MTT assay. The assay is based on the reduction of soluble tetrazolium salt by mitochondria of viable cells. The reduced product, an insoluble purple-colored formazan, is dissolved in dimethyl sulfoxide and measured spectrophotometrically (570 nm). The amount of formazan formed is proportional to the number of viable cells. Cells (3 × 103) are seeded in each of the 96 microplate wells in a 200 μL medium containing the corresponding concentration of daphnetin. Daphnetin is tested at five concentrations (12.5 μM, 25 μM, 50 μM, 100 μM, 200 μM). After 24-hour, 48-hour, and 72-hour exposure, the percentage of proliferative inhibition of treated cells is estimated against the solvent-treated control cells (PI% = [(T/C) 1] × 100). PI = proliferation inhibition; T = treated, C = control. IC50 is calculated from the least square concentration-response regressions.(Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Daphnetin, Daphnetol, 7,8-Dihydroxycoumarin, A2780 cells, AMP-activated protein kinase, Akt, Caspase, Bcl-2 Family, Autophagy, Apoptosis, AMPK, inflammation, mTOR, inhibit, PARP, Parasite, Epidermal growth factor receptor, ErbB-1, EGFR, Inhibitor, HER1, Mammalian target of Rapamycin, schizontocidal, poly ADP ribose polymerase, Protein kinase C, Protein kinase B, protein kinase, Protein kinase A, PKC, PKB, PKA, Reactive Oxygen Species

Compound Identifiers

PubChem CID

5280569