Radicicol (RAD) is a 14-membered resorcylic acid lactone biosynthesized mainly by fungi, originally known as an antifungal antibiotic and later as a potent Hsp90 (heat shock protein 90) inhibitor with diverse bioactivities. The current work aimed to provide a comprehensive review of RAD, including its pharmacological activities and mechanisms of action, as well as its sources, biosynthesis, isolation, and characterization. RAD possessed potent anticancer activity mediated by high-affinity inhibition of Hsp90. By disrupting the stability of oncogenic client proteins such as Raf-1, HER2, and Akt, RAD modulated key signaling pathways, induced apoptosis, and suppressed tumor progression. It also augmented the efficacy of chemotherapeutics and radiotherapy and targeted additional enzymes like ATP citrate lyase and topoisomerase II. Additionally, it demonstrated notable anti-inflammatory, anti-obesity, antiparasitic, antifungal, and antiviral capacities. These findings highlight RAD's significance as a multifunctional therapeutic scaffold for treating cancer and other disorders.