PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), exhibiting inhibitory potency with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. Additionally, it inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts and diminishes AKR1B1-mediated sorbitol accumulation, contributing to the management of blood glucose levels and the inhibition of type 2 diabetes mellitus (T2DM) development [1].

PTP1B/AKR1B1-IN-1（化合物6f）对PTP1B和AKR1B1的抑制作用呈现显著亲和力，其K i 值分别为4.6 μM与0.08 μM。在与PTP1B/AKR1B1-IN-1（20 μM；24小时）处理过的分化的小鼠C2C12细胞中，该化合物仅表现出极低的细胞毒性[1]。同一条件下，该化合物能促进胰岛素（10 μM；15分钟）加强C2C12细胞中Akt磷酸化水平的提升[1]。此外，PTP1B/AKR1B1-IN-1（2 μM；24小时）显著降低了在B3人晶状体上皮细胞系（HLE）中由75 mM D-葡萄糖诱导24小时所导致的山梨醇积累[1]。