The diisonitrile copper chelator SF2768 biosynthesized by Streptomyces thioluteus functions as a chalkophore that transports extracellular copper into producer cells in a complexed form. It was demonstrated that the treatment of eight bacteria, including Bacillus subtilis and Acinetobacter baumannii, with SF2768 led to a moderate growth inhibition which is associated with an increased level of reactive oxygen species (ROS). In addition, SF2768 and its diisonitrile analogues proved to be effective tyrosinase inhibitors. Three new analogues, SF2768 I, K, and L, were identified by detailed spectroscopic analysis.