BPK-29 is a novel, potent and selective ligand of NR0B1 that covalently binds to NR0B1 Cys 274 and inhibits the NR0B1-SNW1 interaction. NR0B1 is an atypical orphan nuclear receptor. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells. It inhibits the anchorage-independent growth of
KEAP1-mutant cancer cells.