KS106

KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Aldehyde Dehydrogenase (ALDH)

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

IC50: 334 nM (ALDH1A1); 2137 nM (ALDH2); 360 nM (ALDH3A1)[1]

KS106 (compound 3h) (0-100 µM; 72 h) shows anti-proliferative activity with IC50s of 5.7, 5.7, 5.7, 4.9, 1.5, 2.6, 1.6, 1.7, 2.2, 20.7 µM for UACC 903, 1205 Lu, HCT116, HT29, NCIH929, U266, RPMI8226, MM.1R, MM.1S, FF2441 cells, respectively[1]. KS106 (5 µM, 24 h) induces apoptosis and cell cycle arrest at the G2/M phase[1]. Apoptosis Analysis[1] Cell Line: HCT116, HT29 cells Concentration: 5 µM Incubation Time: 24 h Result: Induced cell apoptosis. Cell Cycle Analysis[1] Cell Line: HCT116 cells Concentration: 5 µM Incubation Time: 24 h Result: Induced cell cycle arrest at G2/M phase.

[1]. Dinavahi SS, et al. Design, synthesis characterization and biological evaluation of novel multi-isoform ALDH inhibitors as potential anticancer agents. Eur J Med Chem. 2020 Feb 1;187:111962.