TX1-85-1 is a potent, selective, irreversible and covalent inhibitor of pseudokinase Her3 (ErbB3) with IC50 of 23 nM in FRET-based binding assay.
TX1-85-1 covalently modifies Cys721 of Her3 in vitro and in cells.
TX1-85-1 is insufficient to inactivate the Her3/PI3K/AKT pathway explaining lack of growth inhibition for Her3 dependent cells.
TX1-85-1 arrested cell proliferation, inhibited the in vitro tumorigenicity, and lead to loss of stemness in the conversion of induced pluripotent stem cells (iPSCs) into cancer stem cells (CSCs).
