LMTK3 inibitor C28 is a potent, ATP-competitive small-molecule inhibitor of lemur tyrosine kinase 3 (LMTK3) with IC50 of 67 nM.
LMTK3 inibitor C28 displays high selectivity for LMTK3, only 18 of 140 kinases was reduced >50% in the presence of 1 μM, 4 kinases (CLK, 5 nM; DYRK1α, 6 nM; HIPK2, 48 nM; and IRAK4, 41 nM) have IC50 values of <50 nM.
LMTK3 inibitor C28 promotes proteasome-mediated degradation of LMTK3, an HSP90 client protein.
LMTK3 inibitor C28 exhibits potent anticancer activity in different human cancer cell lines (BC cells IC50=6.5-8.4 uM).
LMTK3 inibitor C28 inhibits tumor growth in orthotopic and transgenic mouse models of BC.
