Recently, researchers have studied the functional components and pharmacological effects of Sanghuang (Inonotus hispidus). Simultaneously, Sanghuang tea, Sanghuang wine, and other series of Sanghuang products are produced accordingly, and the development of Sanghuang related industries demonstrates a rapid development trend. Structurally, these compounds are predominantly polysaccharides, polyphenols, steroids, fatty acids, and other metabolites with antitumor, immune regulatory, sleep improvement, antioxidant, and other pharmacological activities. Among these, the antitumor pharmacological effects of I. hispidus are the most prominent. In this paper, the modern research achievements of I. hispidus were reviewed from the aspects of chemical composition, pharmacological activity, related product introduction, and the application prospects of I. hispidus in the field of health and future foods to offer a reference for making complete use of its healthcare value and sustainable and healthy development of its resources. According to this review, I. hispidus could be a promising bioactive compounds source for health promotion and functional foods development.