Elevated levels of reactive oxygen species (ROS) in cancer cells, arising from their altered metabolism, represent a distinctive therapeutic target. Here, we introduce the first example of bisboronic esters as potent agents for rapidly disrupting redox homeostasis, selectively inducing oxidative stress to eliminate cancer cells. Structure-activity relationship studies revealed that both the electronic and steric factors significantly influence their cytotoxicity, with the most effective compounds achieving IC50 values as low as 0.63 mu M. Confocal imaging confirmed the rapid intracellular depletion of ROS, leading to a severe metabolic imbalance and efficient cancer cell death. This study highlights the potential of boronate-based therapeutics for redox-targeted cancer therapy, which may provide a promising foundation for the development of innovative anticancer strategies.