SB-265610

SB-265610 is a potent, selective, nonpeptide small molecule that acts as an allosteric antagonist and inverse agonist of the CXC chemokine receptor 2 (CXCR2). Developed by GSK, it binds to a site distinct from the agonist binding region, effectively preventing receptor activation and subsequent neutrophil chemotaxis. It demonstrates high selectivity for CXCR2 over the closely related CXCR1 receptor. In preclinical models, SB-265610 has been utilized to study inflammatory conditions, such as hyperoxia-induced lung injury and the role of myeloid-derived suppressor cells (MDSCs) in the metastasis of KRAS-mutant colorectal cancer. It is currently used exclusively as a research tool and has not been approved for clinical use in humans.