LCB 03-0110

LCB 03-0110 is a potent, ATP-competitive inhibitor of Discoidin domain receptor (DDR) family and c-Src tyrosine kinase family, as well as Btk and Syk; potently inhibits the activated tyrosine kinase activity of DDR2 (IC50=6 nM), and nonactivated form of DDR2 (IC50=145 nM); suppresses collagen-induced autophosphorylation of DDR1 and DDR2 with IC50 of 164 and 171 nM in cell-based assays; inhibits all eight Src family kinases with IC50 of 2-20 nM; suppresses the proliferation and migration of primary dermal fibroblasts induced by TGF β1 and type I collagen (IC50=194 nM), inhibits cell migration and nitric oxide, iNOS, COX2, and TNF-α synthesis in LPS-activated J774A.1 macrophage cells; suppresses hypertrophic scar formation in wound healing models.

References 1. Sun X, et al. J Pharmacol Exp Ther. 2012 Mar;340(3):510-9. 2. Jung SH, et al. Br J Dermatol. 2013 Jan;168(1):112-9. 3. Kim BH, et al. Exp Dermatol. 2015 Jul;24(7):503-9. View Related Products by Target Discoidin Domain Receptor (DDR)