PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B ( PTP1B ) and aldose reductase ( AKR1B1 ), with IC 50 s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC 50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels.