MP-1 is a covalent inhibitor of fumarate hydratase (FH) that exhibits cytotoxicity dependent on FH. MP-1 engages a functional cysteine in the Zn-finger domain of the tRNA methyltransferase enzyme TRMT1.
XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.