Purple Perilla (Perilla frutescens (L.) Britt.) is an annual herb commonly used as a traditional Chinese medicine for more than 1000 years. This work investigated the chemical composition, insecticidal and repellent activities of the essential oil of Purple Perilla aerial parts against Lasioderma serricorne (Fabricius). Moreover, we also isolated active constituents from the essential oil. The experiment was investigated in 2013 in Beijing. The essential oil of Purple Perilla was obtained by hydrodistillation and a total of 47 components in the essential oil were identified with GC–MS. It was found that the main compounds included carvone (32.55%), perilla aldehyde (20.52%), caryophyllene (9.85%), 2-furyl methyl ketone (7.53%), 2,6-dimethyl-6-(4-methyl-3-pentenyl)-2-norpinene (5.17%), and β-terpinyl acetate (3.41%). With a further isolation, four active constituents were obtained from the essential oil and identified as R-(+)-carvone, perilla aldehyde, 2-furyl methyl ketone, and β-caryophyllene. In the progress of assay, it showed that the essential oil, R-(+)-carvone, perilla aldehyde, and 2-furyl methyl ketone exhibited stronger insecticidal and repellent activities against L. serricorne than β-caryophyllene. The results indicate that the essential oil of Purple Perilla aerial parts and isolated compounds have potential for development into natural insecticides or repellents for control of insects in stored products.