The Keap1–Nrf2 pathway plays a crucial role in protecting aerobic cells from the damaging effects of reactive oxygen intermediates and toxic electrophiles, which are major causes of neoplastic and chronic degenerative diseases. This pathway is transcriptionally regulated and can be activated by various exogenous and endogenous small molecules (inducers). Inducers react with cysteine residues in the sensor protein Keap1, leading to the stabilization and nuclear translocation of the transcription factor Nrf2. This results in the coordinated upregulation of genes coding for cytoprotective proteins. Additionally, inducers inhibit pro-inflammatory responses, and there is a strong correlation between inducer concentration and anti-inflammatory activity. Genetic deletion of Nrf2 increases sensitivity to electrophiles, oxidants, and inflammatory agents, while activation of the Keap1–Nrf2 pathway enhances survival and adaptation under stress conditions. The pathway also interacts with other signaling pathways, influencing fundamental biological processes such as proliferation, apoptosis, angiogenesis, and metastasis.The Keap1–Nrf2 pathway plays a crucial role in protecting aerobic cells from the damaging effects of reactive oxygen intermediates and toxic electrophiles, which are major causes of neoplastic and chronic degenerative diseases. This pathway is transcriptionally regulated and can be activated by various exogenous and endogenous small molecules (inducers). Inducers react with cysteine residues in the sensor protein Keap1, leading to the stabilization and nuclear translocation of the transcription factor Nrf2. This results in the coordinated upregulation of genes coding for cytoprotective proteins. Additionally, inducers inhibit pro-inflammatory responses, and there is a strong correlation between inducer concentration and anti-inflammatory activity. Genetic deletion of Nrf2 increases sensitivity to electrophiles, oxidants, and inflammatory agents, while activation of the Keap1–Nrf2 pathway enhances survival and adaptation under stress conditions. The pathway also interacts with other signaling pathways, influencing fundamental biological processes such as proliferation, apoptosis, angiogenesis, and metastasis.