Purpurin is a naturally occurring anthraquinone isolated from the roots of Rubia cordifolia. Historically, it has been used as a red dye. However, its photosensitizing property and biological effects have deciphered its novel application. Purpurin shows antigenotoxic, anticancer, neuromodulatory, and antimicrobial potential associated with antioxidant action in in vivo and in vitro experiments. A robust antioxidant nature of purpurin is responsible for the majority of its pharmacological effects. It produces anti‐inflammatory activity by reducing oxidative stress, which is a fundamental property to target diseases involving endoplasmic reticulum and mitochondrial stress. It can cross the blood–brain barrier and produce neuroprotective effects, including antidepressant and anti‐Alzheimer action. It shows antimutagenic property via inhibiting essential CYP‐450 enzymes. Interestingly, it gets photosensitized by UV‐light and produces target‐specific ROS‐dependent apoptosis in cancer cells. Therefore, it owns cell killing and cell survival potential subject to the influence of external conditions. Hitherto, limited research studies are performed with purpurin to understand its therapeutic potential. Hence, this review describes and discusses different in vivo, in vitro, and in silico studies performed using purpurin. It also covers physicochemical, pharmacokinetics, and toxicology aspects of purpurin. Moreover, in the end, the prospect of purpurin in the management of cancer has also been proposed.