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BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells[1].

BPK-29 hydrochloride substantially engages NR0B1 with good overall proteomic selectivity in KEAP1-mutant Non-Small Cell Lung Cancers[1].

[1]. Bar-Peled L, et al. Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer. Cell. 2017 Oct 19;171(3):696-709.e23.