In the past decades, several steroids and their derivatives were found to possess moderate to good PTP1B inhibitory activities, such as lithocholic acid (LCA, 1, Figure 1) [11], claramine (3) [12] and trodusquemine (2) [13], the first PTP1B inhibitor for the treatment of diabetes in clinical trials. This evidence concerns the gene PTPN1 and diabetes mellitus.