XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 12.9 nM and 38.1 6.9 nM against MST1 and MST2, respectively. XMU-MP-1 also reduces the phosphorylation of LATS1/2, and YAP by inhibiting MST1/2 kinase activities.
XMU-MP-1 is on-target to MST1/2. XMU-MP-1 block MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM).
XMU-MP-1 displayed excellent in vivo pharmacokinetics and is 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. XMUMP-1 treatment exhibit substantially greater repopulation rate of human hepatocytes in the Fah-deficient mouse model than in the vehicle-treated control, indicating that XMU-MP-1 treatment might facilitate human liver regeneration.
XMUMP-1 is dissolved in 0.1% citric acid aqueous solution containing 20% Kolliphor HS 15.