Dual DDR1 and DDR2 inhibitor 5n

Dual DDR1 and DDR2 inhibitor 5n is a highly potent, selective, dual Discoidin domain receptor DDR1 and DDR2 inhibitor with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively; displays significant selectivity against a panel of 403 wild-type kinases at 1 uM (Abl1 IC50=494 nM); dose-dependently inhibited lipopolysaccharide (LPS)-induced interleukin-6 (IL-6) release in mouse primary peritoneal macrophages (MPMs), attenuates lung pathophysiologic changes in LPS-challenged mice, effectively decreases the levels of TNF-α and IL-6 both in BALF and serum.

References 1. Wang Z, et al. J Med Chem. 2018 Aug 3. doi: 10.1021/acs.jmedchem.8b01045. View Related Products by Target Discoidin Domain Receptor (DDR)