Molecular Weight(MW): 178.14
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.
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|Description||Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.|
Daphnetin strongly inhibits not only EGF receptor-catalyzed tyrosine phosphorylation of exogenous substrate but also PKA and PKC activities.  Daphnetin inhibits MCF-7 estrogen-responsive human carcinoma cell line at 24-hour exposure with IC50 of 73 μM. Daphnetin reduces the level of cyclin D1 even at 50 μM.  Daphnetin protects the cortical neurons against dexamethasone-induced reduction of cell viability in a dose-dependent manner.  Daphnetin inhibits the activities of endogenous or recombinant TaPRK in a specific and dose-dependent manner.  daphnetin causes a 50% inhibition (IC50) of 3H-hypoxanthine incorporation by Plasmodium falciparum at concentrations between 25 μM and 40 μM.  Daphnetin inhibits the mitogenic signalling of ERK1/ERK2. 
|In vivo||Daphnetin at 140 mg/kg significantly decreases uterine weights by 39.5%.  Two and 8 mg/kg administration of Daphnetin could improve the performance of stress mice in Morris water maze tests and forced swimming tests.  Daphnetin significantly prolongs survival of P. yoelli-infected mice. |
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
-  Yang EB, et al. Biochem Biophys Res Commun, 1999, 260(3), 682-685.
-  Jiménez-Orozco FA, et al. Eur J Pharmacol, 2011, 668(1-2), 35-41
-  Liao MJ, et al. Fundam Clin Pharmacol, 2012.
|In vitro||DMSO||35 mg/mL (196.47 mM)|
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