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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Product Description
Information
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibitsEGFR,PKAand PKC withIC50of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities. In vitro
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. Cell Data
