AKR1B10-IN-1

AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase

3.5 nM (AKR1B10); 277 nM (AKR1B1)[1]

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.

[1]. Endo S, et al. Synthesis of Potent and Selective Inhibitors of Aldo-Keto Reductase 1B10 and Their Efficacy against Proliferation, Metastasis, and Cisplatin Resistance of Lung Cancer Cells [published correction appears in J Med Chem. 2018 Feb 8;61(3):1380]. J Med Chem. 2017;60(20):8441-8455.