H052 is a selective inhibitor of Staphylococcus aureus α-hemolysin (Hla). It binds to the Hla monomer, disrupting its interaction with the host cell membrane, thereby blocking pore formation and inhibiting calcium influx, cytotoxicity, and inflammatory response. H052 exhibits inhibitory activity against Hla-induced calcium influx (EC50 = 30 nM in U937 cells) and holds potential for research into lung infections caused by S. aureus.