PD-L1/LpxC-IN-1

PD-L1/LpxC-IN-1 (Conpound 12b) is the inhibitor for PD-L1 and LpxC with IC50 of 5.2 μM and 0.081 μM. PD-L1/LpxC-IN-1 inhibits the biosynthesis of bacterial lipopolysaccharide, causes the lysis and death of bacterial cells. PD-L1/LpxC-IN-1 inhibits Gram-negative bacteria, MIC for K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028 and P. aeruginosa ATCC 9027 is 0.25-0.5 μg/mL. PD-L1/LpxC-IN-1 downregulates the expression of inflammatory factors IL-2 and IFN-γ, upregulates the expression of CD4+ and CD8+ cells, thereby activating the immune system and inhibiting excessive inflammatory responses. PD-L1/LpxC-IN-1 exhibits antibacterial activity in K. pneumoniae ATCC 13883 infected mouse models[1].