Chemical investigation of one entomopathogenic fungus Paecilomyces cateniobliquus YMF1.01799 led to the isolation and identification of six metabolites, which include three new compounds (2-3, and 5) and three known metabolites. Their structures were established by spectroscopic studies such as 1D and 2D NMR and MS analysis. Insect growth experiments suggested that polyketide-derived compound 1 showed significant inhibitory effect on the growth of cotton bollworm Helicoverpa armigera, while terpenoid-derived metabolite 5 promoted the growth of the larvae. The findings revealed that the entomopathogenic fungus P. cateniobliquus could produce different types of metabolites to regulate growth of the insect.