Disclosed are a metal nanoparticle onto which a peptide substrate specifically degraded by protease and fluorophore are chemically modified for selectively imaging protease expressed in cell and in tissue in a human body, and the use thereof. Also, a quantitative analysis method of protease using the metal nanoparticle, a cell imaging method and a drug screening method of inhibiting a protease overexpression are provided. In detail, the present invention is directed to a metal nanoparticle having a peptide substrate and fluorophore coupled thereto, the peptide substrate and the fluorophore being specifically degraded by due to a protease activated in various ways in cell and in a human body to exhibit fluorescence. Hence, the metal nanoparticle can be used to rapidly screen activation and inhibition of the protease in the imaging manner. Also, the metal nanoparticle is capable of being selectively absorbed into a cell and a tissue so as to be possibly used as a sensor for real-time cell imaging and early diagnosis of non-invasive diseases.