Insects constitute the largest and most diverse group of animals on Earth. They also serve as the hosts or nutrient sources for an immense assemblage of parasites, pathogens, and predators, ranging from bacteria and fungi to plant and animals. More than 700 known fungal species from 100 genera have adopted an entomopathogenic lifestyle. These fungi are widely distributed, occurring in aquatic, forest, and agricultural habitats, and are often used as active ingredients in microbial insect pest control agents. Their mode of action against insects involves the attachment of conidia to the insect cuticle, followed by germination, cuticle penetration, and internal dissemination throughout the insect. During this process, secreted enzymes, protein toxins, and secondary metabolites can be used by the fungus to overcome the host immune system, modify host behavior, and defend host resources against competing pathogens and saprophytes. In some cases, the host insect relationship has been found to be associated with bioactive fungal metabolites. These metabolites exhibit a wide variety of insecticidal, antibacterial, antifungal, anticancer, antioxidant, and antiviral activities. Using molecular techniques and phylogenetic analyses, both the asexual (anamorphic) stages and sexual (teleomorphic) stages of entomopathogenic fungi have recently been shown as linked together. Therefore, entomopathogenic fungi, especially in complex with the host insect, might be a promising source of bioactive molecules of pharmaceutical and various industrial interests. Here, we evaluated the antimicrobial activity of entomopathogenic fungi metabolites against plant pathogenic bacteria and fungi for the use in agriculture. The radicals scavenging activity and the anticancer activity were also evaluated for pharmaceutical interests.