The ingestion of some organic compounds has been known to lower the risk of cancer. With emerging studies in the past decade, the biological effect of these compounds has been recognized within a clinical context and presents an appealing strategy for cancer prevention. These compounds, now commonly referred as chemopreventive agents or anticarcinogens, often exert their activity by inducing expression of phase II enzymes and endogenous antioxidants via the Nrf2 signaling pathway, which defends cells from harmful oxidative stress and reactive carcinogenic intermediates. Here, we present several micro- and nanoscale technological modularities, including two molecular assays and a multiplexed microOuidic device, toward the creation of a nanoengineered platform for high-throughput screening of chemopreventive compounds targeting Nrf2. The ability to rapidly identify agents that can prevent the occurrence and reduce the severity of cancer is of great importance in the management of cancer and represents a pathway toward the realization of preventive medicine.