XMU-MP-2 is a potent and selective BRK/PTK6 (breast tumor kinase) inhibitor with biochemical IC50 of 3.2 nM.
XMU-MP-2 inhibits the autophosphorylation of BRK Y342 in dose-dependent manner (maximum inhibition at 500 nM), abolishes phosphorylation levels of STAT3 Y705 and STAT5 Y694.
XMU-MP-2 blocks proliferation and survival of BRK-transformed Ba/F3 cells with IC50 of 29.7 nM.
XMU-MP-2 cooperates strongly with HER2 inhibitor or ER blockade to block breast cancer cell proliferation in vitro and in vivo.
