GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity ( DC 50 =0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities ( IC 50 =4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer . (Pink: BRD4 ligand ( HY-129939 ); Blue: VHL ligand ( HY-123109 ); Black: linker ( HY-W013253 )).
Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Epigenetics | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Epigenetic Reader Domain
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