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Daphnetin

Catalog No. T2851 CAS 486-35-1

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

Daphnetin, 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

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Daphnetin, 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, PKA:9.33 μM, PKC:25.01 μM
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)

Synonyms	Autophagy, PARP, PKA, Daphnetin, 7,8-Dihydroxycoumarin, A2780 cells, mTOR, Protein kinase A, Inhibitor, Caspase, poly ADP ribose polymerase, PKB, inflammation, schizontocidal, Epidermal growth factor receptor, Protein kinase C, Reactive Oxygen Species, HER1, Bcl-2 Family, Parasite, Protein kinase B, Akt, Mammalian target of Rapamycin, AMPK, Apoptosis, protein kinase, ErbB-1, inhibit, AMP-activated protein kinase, PKC, EGFR, Daphnetol
Molecular Weight	178.143
Formula	C9H6O4
CAS No.	486-35-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 33 mg/mL (185.2 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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 Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library GPCR Compound Library Cytokine Inhibitor Library Anti-Cardiovascular Disease Compound Library Traditional Chinese Medicine Monomer Library TGF-beta/Smad Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library

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