CH6824025 is a potent, selective discoidin domain receptor 1 (DDR1) inhibitor, dose-dependently inhibits the phosphorylation of DDR1 induced by adding Type 1 collagen to U2OS cells stably expressing DDR1 with IC50 of 8.9 nM.
CH6824025 is highly selective, because the 451 types of kinases evaluated by KINOMEscan, only
DDR1, DDR2, and Lymphocyte-Oriented Kinase (LOK) showed more than 99% competitive
binding inhibition at 1 uM.
CH6824025 suppresses the phosphorylation of DDR1 in the kidney, and the amount of hydroxyproline, the Sirius red- and the F4/80-positive area.
CH6824025 significantly decreases the mRNA expression of fibrosis and inflammation-related genes in the kidney were significantly decreased.
CH6824025 could ameliorate fibrosis and inflammation in unilateral ureteral obstruction (UUO) mice.
CH6824025 inhibits cell motility (e.g., migration) that prevents the progression of fibrosis and improves mitochondrial function in UUO mice.