Countless bioactive constituents obtained from different medicinal plants have long been focused by the researchers of the scientific community and pharmaceutical industry. In recent years, extensive in vitro and in vivo research has been carried out with these biomolecules to develop complementary and alternative medicines. Findings revealed that these molecules may act as promising agents for almost all kinds of pathophysiological states. Further, these novel bioactive compounds are mostly not harmful in dietary doses. In this eclectic review, we highlighted the beneficial role of genistein, an isoflavone available mainly in the legumes particularly in soybean. Genistein is a potent phytoestrogen which binds with both alpha and beta estrogen receptors and regulate the divergent intracellular signaling cascades of estrogen. It also has the potential to competitively inhibit different imperative ATP utilizing enzymes. These properties help genistein in regulating various cellular and biochemical functions at different levels of structural organization in the body. Moreover, it’s very low cytotoxicity and abundance in regular aliment compared to other isoflavones makes it a more promising therapeutic option. Emerging evidence from the literature proves the competence of genistein in combating oxidative stress, cancer, diabetes, obesity, inflammation, osteoporosis, neuropathy and some other disorders. This review aims to unravel the assorted underlying mechanisms behind the multivariate properties of this unique aglycone.