Insects are the most abundant and diverse animal class on earth and they are associated with an amazing variety of microorganisms. The ability of insects to live in unique niche habitats is often facilitated by their associated microbe, which perform many important host functions, especially against pathogens, parasitoids or predators by producing metabolites and the enormous insect-associated microbial communities are a potential source of novel antibiotic metabolites. To find more insect-associated microorganisms-derived bioactive metabolites, the study of the carpenter ants-associated microorganisms was carried out and a strain Streptomyces sp. 1H-GS5 exhibiting good activities against some lines of tumor cell was obtained. In the further investigation of chemical components from the broth of Streptomyces sp. 1H-GS5, a new spectinabilin derivative (1) along with the known compound, spectinabilin (2) (Figure 1), were isolated. Here the report deals with the details of the isolation, structure elucidation and the bioactivity of the new compound.