Fig. 1.

Discovery of IHMT-MST1-39 as a potent and selective MST1 inhibitor. a The chemical structure of IHMT-MST1-39. b ADP biochemical assay determination of IC₅₀ of IHMT-MST1-39 and XMU-MP-1 against MST1 at different compound concentrations. c, d IC₅₀ and KD values of IHMT-MST1-39 against different MST isoforms. Data were expressed ± SEM from three independent experiments (n = 3). e The KINOME-scan result of IHMT-MST1-39 against a panel of 468 kinases. f Molecular modeling analyses of the binding mode of MST1 with IHMT-MST1-39. MST1 homology model, template PDB code:6yat. g Inhibitory effects against the phosphorylation of MOB1, LATS1 in rodent pancreas cell lines after treatment of compound for 2 h. h YAP-TEAD reporter activity was measured in MDA-MB-231 cells exposed to high glucose, and then treated with compound at different time, compound activities were compared to high glucose control