Glutathionyl ferrocene (GSH-Fc) was synthesized from glutathione and ferrocenyl amine using O-(benzotriazol-yl)-N,N,N',N'-tetramethyluronium(HBTU)/1-hydroxybenzotrizole (HOBT) as coupling agents in solution with a yield of 23.2%. The compound was characterized by 1H-NMR, IR and MS. Interactions of bovine serum albumin (BSA) with glutathionyl ferrocene were investigated by electrochemical methods. Experimental results revealed that there were specific interactions between BSA and GSH-Fc at the IIA subdomain. The binding constant and binding sites were obtained by linear sweep voltammetry and had values of 1.71×106 L·mol-1 and 1.30, respectively. Fluorescence spectroscopy methods were employed to investigate the interaction between GSH-Fc and BSA as well. Results showed that the fluorescence of BSA was quenched by GSH-Fc during a static quenching process. The binding constant and the number of binding sites were obtained and had values of 2.74×106 L·mol-1 and 1.57, respectively, which agreed well with results fromelectrochemical experiments.