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<i>Inonotus hispidus</i> mushroom is a popular edible and medicinal mushroom with a long history of use. It is well known as a medicinal fungus with various health benefits for its significant anticancer and immunomodulatory activities. Over the last 60 years, secondary metabolites derived from <i>I. hispidus</i> and their biological activities have been discovered and investigated. Structurally, these compounds are mainly polyphenols and triterpenoids, which have anticancer, anti-inflammatory, antioxidant, antimicrobial, and enzyme inhibitor activities. Here, the secondary metabolites derived from <i>I. hispidus</i> and their activities were systematically and comprehensively classified and summarized, and the biosynthetic pathway of stylylpyrones was deduced and analyzed further. This review contributes to our understanding of <i>I. hispidus</i> and will help with research into natural product chemistry, pharmacology, and the biosynthesis of <i>I. hispidus</i> metabolites. According to this review, <i>I. hispidus</i> could be a promising source of bioactive compounds for health promotion and the development of functional foods.