KS100

KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 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: 230 nM (ALDH1A1); 1542 nM (ALDH2); 193 nM (ALDH3A1)[1]

KS100 (compound 3j) (0-100 µM; 72 h) shows anti-proliferative activity with IC50s of 3.7, 2.1, 2.9, 2.5, 0.3, 1.0, 1.2, 1.3, 2.1, 9.8 µM for UACC 903, 1205 Lu, HCT116, HT29, NCIH929, U266, RPMI8226, MM.1R, MM.1S, FF2441 cells, respectively[1]. KS100 (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. Apoptosis 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.