AKR1B10-IN-1, a powerful AKR1B10 (Aldo-Keto Reductase 1B10) inhibitor, demonstrates an IC50 value of 3.5 nM. This compound effectively curtails the proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells.

AKR1B10:3.5 nM , AKR1B1:277 nM

AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) dose-dependently suppresses the growth of both A549 and A549/1B10 cells[1]. AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) completely suppresses increased cell proliferation by the overexpressing AKR1B10 as well as the endogenous protein[1]. AKR1B10-IN-1 (compound 4e) (0-40 μM; 26 hours; pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours) decreases the cell viability of CDDP-R-A549 cells in a dose-dependent manner[1]. Cell Viability Assay[1]Cell Line: A549 cells, A549/1B10 cells (AKR1B10-stably overexpressing A549 cells) Concentration: 0, 10, 20?μM Incubation Time: 96 hours Result: Dose-dependently suppressed the growth of both A549 and A549/1B10 cells, and statistically significant at 20 μM. Cell Viability Assay[1]Cell Line: CDDP-resistance (cisplatin-resisitance) of A549 cells Concentration: 0, 10, 20, 40?μM Incubation Time: Pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours Result: Decreased the cell viability of CDDP-R-A549 cells in a dose-dependent manner, and most obvious in the treatment of 40 μM.