Daphnetin (DAP), a natural coumarin derivative isolated from Chinese medicinal herbs, possesses abundant biological activities, such as anti-inflammatory, antioxidant, antimalarial and anti-arthritic. Experiments on mice have shown, that DAP exerts neuroprotective and anti-inflammatory effects, and the potential mechanism is involved the inhibition of TLR4/NF-κB mediated inflammatory signaling pathway. Besides, DAP, a multi-targeted medication, can have the application for the anti-angiogenesis and cancer therapy, through the inhibition of the IKKs/IκBα/NF-κB, Src/FAK/ERK1/2 and Akt signaling pathways. It is known, that protein kinases play key roles in the control of cell proliferation, differentiation, and metabolism. Daphnetin inhibits tyrosine-specific protein kinase, EGF receptor, serine/threonine-specific protein kinases, including cAMP-dependent protein kinase (PKA) and protein kinase C (PKC).