WRG-28 (DDR2 inhibitor WRG-28) is a potent, selective, allosteric inhibitor of discoidin domain receptor 2 (DDR2) with binding IC50 of 230 nM.
WRG-28 bluntsd collagen I-mediated DDR2 tyrosine phosphorylation, ERK activation, and SNAIL1 protein stabilization (IC50=286 nM) in HEK293 cells expressing DDR2, without effect on normal mammary epithelial MCF10A cells.
WRG-28 displays no activity against collagen I-induced tyrosine phosphorylation of the related DDR1 RTK in HEK293 cells.
WRG-28 inhibits DDR2-collagen interaction in an allosteric manner, inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs.
