MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.
MR-2088 displays a relatively clean kinome-wide profile with an S (35) selectivity score of 0.295 against 97 diverse human kinases and disease-relevant mutants at 1 uM.
MR-2088 inhibits the phosphorylation of ATG13 Ser 318 and prevents the degradation of p62 with EC50 36 nM and 48 nM for inhibiting downstream phosphorylation of ATG13 under starved and trametinib-treated conditions, respectively.
MR-2088 blocks autophagy flux, exhibits synergistic antiproliferative activity with MEK inhibition.
