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Daphnetin

Catalog No. T2851 CAS 486-35-1

Synonyms: 7,8-Dihydroxycoumarin, Daphnetol

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

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Daphnetin, CAS 486-35-1

Pack Size	Availability	Price/USD
10 mg	In stock	$ 43.00
25 mg	In stock	$ 87.00
50 mg	In stock	$ 169.00
100 mg	In stock	$ 256.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.82%

Purity: 99.8%

Purity: 98.33%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.
Targets&IC50	EGFR:7.67 μM, PKC:25.01 μM, PKA:9.33 μM
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.
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.
Kinase Assay	Assay of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) activities.: PKC and PKA activities are detected. Briefly, 5 mL of PKC or PKA is mixed with 5 mL of lipid preparation containing 100 mM phorbol 12-myristate 13-acetate, 2.8 mg/mL phosphatidyl serine, and Triton X-100 mixed micelles for PKC assay or 5 mL of 40 mM cAMP in 50 mM Tris-HCl, pH 7.5, for PKA assay, and 5 mL of daphnetin. The reaction is started by adding 10 mL of PKC substrate solution containing 250 mM acetylated myelin basic protein, 100 mM ATP, 5 mM CaCl2, 10 mM MgCl2, 20 mM Tris-HCl, pH 7.5, or 10 mL of PKA substrate solution containing 200 mM Kemptide, 400 mM ATP, 40 mM MgCl2, 1 mg/mL BSA, 50 mM Tris-HCl, pH 7.5, and 20-25 mCi/mL[g-32P] ATP. After incubation at 25 °C for 5 minutes, 20 mL of each mixture is spotted on a piece of phosphocellulose disc which is immediately put into 1% H3PO4. After free [g-32P] ATP on the discs is removed, the peptide-incorporated 32P on the discs is counted in a scintillation counte
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)
Source	Natural Products > Thymelaeaceae > daphne

Synonyms	7,8-Dihydroxycoumarin, Daphnetol
Molecular Weight	178.14
Formula	C9H6O4
CAS No.	486-35-1

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 33 mg/mL (185.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Yang EB, et al. Biochem Biophys Res Commun, 1999, 260(3), 682-685. 2. Jiménez-Orozco FA, et al. Eur J Pharmacol. 2011 Oct 1;668(1-2):35-41. 3. Liao MJ, et al. Fundam Clin Pharmacol, 2012. 4. Kane K, et al. Biochem Cell Biol, 2012, 90(5), 657-666. 5. Yang YZ, et al. Am J Trop Med Hyg, 1992, 46(1), 15-20. 6. Lv H, et al. Daphnetin-mediated Nrf2 antioxidant signaling pathways ameliorate tert-butyl hydroperoxide (t-BHP)-induced mitochondrial dysfunction and cell death. Free Radic Biol Med. 2017 May;106:38-52.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Kinase Inhibitor Library Antiparasitic Natural Product Library Anti-Cancer Drug Library Inhibitor Library Anti-Parasitic Compound Library Tyrosine Kinase Inhibitor Library TGF-beta/Smad Compound Library FDA-Approved Kinase Inhibitor Library Drug Repurposing Compound Library

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Keywords

Daphnetin 486-35-1 Angiogenesis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Microbiology/Virology Tyrosine Kinase/Adaptors EGFR PKA PKC Parasite PARP A2780 cells mTOR Protein kinase A Inhibitor Caspase poly ADP ribose polymerase PKB inflammation schizontocidal Epidermal growth factor receptor Protein kinase C 7,8-Dihydroxycoumarin Reactive Oxygen Species HER1 Bcl-2 Family Daphnetol Protein kinase B Akt Mammalian target of Rapamycin AMPK Apoptosis protein kinase ErbB-1 inhibit AMP-activated protein kinase inhibitor

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