Objective/Background The genus Diospyros L. (Ebenaceae) includes about 778 species worldwide, with over 500 of them known for their significant health benefits. Among them, Diospyros mollis Griff. has been used as a tonic and treatment for many diseases related to digestive disorders and intestinal parasites. Furthermore, the fruit has also been used for dyeing silk fabrics. The purpose of this comprehensive review is to provide researchers with important information about D. mollis, particularly regarding its chemical composition and biological effects. This information can support current understanding and future studies to develop novel herbal formulations based on this species. Additionally, this review aims to compile and summarize the available literature on this species, covering its botanical, ethnomedicinal, phytochemical, and pharmacological properties reported to date. Methods The relevant information on D. mollis was collected via online electronic and databases, including Scopus, Pubmed, Web of Science, Google Scholar, ScienceDirect, Springer Link, SciFinder, and other scientific databases. Results A comprehensive review of the literature reveals that D. mollis contains various chemical constituents such as naphthalene and naphthoquinone derivatives, triterpenoids, alkaloids, sterols, glycosides, and fatty acid esters isolated from the berry, root, bark, and leaf of this species, with several pharmacological effects and other applications. Many pharmacological effects, such as hyaluronidase inhibitory, anthelmintic, and antiparasitic activities of various extracts and isolated compounds of D. mollis, are reported in this review. The review demonstrates the importance of D. mollis in the treatment of diseases, its application in fabric dyeing techniques, and its traditional use. Conclusion In conclusion, D. mollis emerges as a promising botanical resource with its rich history in traditional medicine and diverse chemical constituents, paving the way for potential future applications and innovations in the field of herbal medicine and drug development.