Upon exposure to GSH, the functional molecules were activated or released from the disassembled nanostructure, exerting their therapeutic or imaging effects: a) the FL intensities of AO-Luc at 547 nm and Zn-PPA-SH at 672 nm were markedly enhanced with a ~500- and ~85.9- fold improvement, respectively, b) the released NLG919 inhibited IDO1, reducing immunosuppressive Tregs, and c) the released Zn-PPA-SH could bind to albumin for robust ROS generation upon light/ultrasound stimulation, inducing a direct tumor-killing effect or augmenting immunological cell death. This evidence concerns the gene IDO1 and neoplasm.