Aquilaria sinensis (Lour.) Spreng. (Thymelaeaceae family), is the fragrant resin-infused wood derived from the wounded trees of Aquilaria species. With years of studies, phytochemical investigations on A. sinensis have been proven to possess various chemical constituents which contained sesquiterpenes and 2-(2-phenylethyl) chromone derivatives as two classes of characteristic compounds. As the medicinal parts, A. sinensis also demonstrates a wide array of pharmacological properties of anti-inflammatory, antioxidative, cytotoxicity activities and showed potential properties for the treatment of depression, and neuroinflammation. As a result, phytochemical investigations on A. sinensis exhibit chemotaxonomic significance, characterizing certain Thymelaeaceae species well. In addition, the latest research progress on A. sinensis was reviewed in order to have a more particular understanding and tap of its potential.