Glutathione S-transferase Pi (GSTpi) is the most important subtribe of GSTs protein superfamily, and plays an important role in the process of detoxification, antioxidant and anti-inflammation. Here we use a GSTpi inhibitor, 6-(7-nitro-2, 1, 3-benzoxadiazol-4-ylthio) hexanol (NBDHEX), to evaluate the effect of GSTpi on the growth of mice. Mice treated with NBDHEX have heavier weight and longer length. But there is no significant difference in ratios of the weights of brain, kidney, lung, spleen, liver and heart to the whole body weight and Lee's index between NBDHEX and control mice. These data suggested that GSTpi might inhibit mouse growth. Enzyme-linked immunosorbent assay (ELISA) showed that GSTpi inhibition induced a significant increase of growth hormone (GH) levels in blood and pituitary and insulin-like growth factor (IGF-1) levels in liver and blood in mice. Further observation demonstrated that GSTpi negatively regulated GH-Janus Kinase 2 (JAK2)-signal transducer and activator of transcription 5 (STAT5) axis through inhibiting STAT5 phosphorylation, and as a result of GSTpi decreased the expression of IGF-1.