ALDH inhibitor KS100 (KS100) is a novel, potent, multi-isoform ALDH inhibitor with IC50 of 207/1410/240 nM for ALDH1A1/ALDH2/ALDH3A1, respectively.
KS100 was mitigated by development of a nanoliposomal formulation, called NanoKS100. NanoKS100 was 5-fold more selective for killing melanoma cells compared with normal human fibroblasts.
Inhibition by KS100 significantly reduced total cellular ALDH activity to increase reactive oxygen species generation, lipid peroxidation, and accumulation of toxic aldehydes leading to apoptosis and autophagy.
