S07-2010 is a potent pan- AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC 50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3 , AKR1C4 , AKR1C1 and AKR1C2 , respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells.