xmu-mp-1

Description: XMU-MP-1 is a potent, reversible and selective inhibitor of MST1/2 with IC50 values of 71.1 nM and 38.1 nM against MST1 and MST2, respectively. XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 inhibits phosphorylation of MOB1 in a dose-dependent manner. Furthermore, with increasing ATP concentration, XMU-MP-1 exhibits a proportional increase in IC50 against MST1/2, as well as an attenuated inhibition of the MST2-mediated phosphorylation of MOB1. The pharmacological modulation of MST1/2 kinase activities provides a novel approach to potentiate tissue repair and regeneration, with XMU-MP-1 as the first lead for the development of targeted regenerative therapeutics.

References: Sci Transl Med. 2016 Aug 17; 8(352):352ra108.