The extensive use of pesticides may negatively affect human health. Additionally, it is one of the main reasons for the decline of pollinators and is thus a hazard for most crops and biodiversity as a whole. Good candidates for the replacement of pesticides with ones less toxic to humans and pollinators are natural products (bioactive compounds extracted from plants), even though it should be kept in mind that some of them can be toxic too. Ailanthus altissima (Mill.), swingle, known also as tree of heaven, (Simaroubaceae) is one of the most aggressive alien invasive plants. It demonstrates a high tolerance to various habitat conditions and a potent propagation ability. This plant has a prominent ability to suppress the seed development of local vegetation. The aim of this review study is to summarize the potential of this plant for use as a natural pesticide, starting with ethnobotanical information. The essential oils extracted from A. altissima with its main components α-curcumene α-gurjunene, γ-cadinene, α-humulene, β-caryophyllene, caryophyllene oxide, germacrene D, etc., have been reported to possess different activities such as insect repellent, insecticidal, and herbicidal activity. Additionally, polar extracts and particularly quassinoids, the phenolic constituents of A. altissima leaves, are potent phytotoxins and fumigants. The basic extraction protocols are also summarized.