XMU-MP-1 is a potent and selective MST1/2 inhibitor with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM, respectively.. XMU-MP-1 blocked MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 displayed excellent in vivo pharmacokinetics and was able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection.