ULK-101 (ULK101) is a potent and selective ULK1 inhibitor with in vitro IC50 of 8.3 nM, inhibits ULK2 with IC50 of 30 nM.
ULK-101 reduces Ser15 phosphorylation in a concentration-dependent manner in cell-based assay (EC50=390 nM), which is more potent than SBI-0206965 showing a cellular EC50 of 2.4 uM.
ULK-101 displays desirable kinome selectivity profile.
ULK-101 suppresses autophagy induction and autophagic flux in response to different stimuli, ULK1 inhibition sensitizes KRAS mutant lung cancer cells to nutrient stress.
