Iberin is an isothiocyanate (ITC) and a sulforaphane homolog that exhibits antioxidative and anticancer chemotherapeutic activity. Like other ITCs, iberin may display chemopreventive potential by inducing phase II enzymes. In vitro, iberin induces Nrf2 nuclear translocation and increases levels of heme oxygenase-1 and glutamylcysteine synthetase, both potentially related to alterations in ERK signaling. Iberin also increases expression of antioxidative enzymes thioredoxin reductase 1 and glutathione peroxidase 2 in cellular models. In cancer cells, iberin induces p21 expression, decreases expression of cyclin-dependent kinases (CDKs) 2, 4, and 6, and increases caspase activity, resulting in apoptosis.