gne 987

GNE-987 is a highly active chimeric BET degrader that binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low-nanomolar affinity and induces exceptionally potent BRD4 degradation in cells, achieving picomolar DC50 values in EOL-1 acute myeloid leukemia cells, thereby serving as a powerful chemical biology tool for dissecting BET-dependent transcriptional regulation.

(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).

PROTAC BRD4 ligand-1 is a PROTAC and a BRD4-targeted inhibitor with BET inhibitory activity. This ligand is cell-permeable and is used for the synthesis of PROTAC GNE-987, possessing antitumor potential.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker conjugate for PAC. PROTAC BRD4 Degrader-5-CO-PEG3-N3 comprises the BRD4 degrader GNE-987 linked through a PEG-based spacer to enable modular bioconjugation. PROTAC BRD4 Degrader-5-CO-PEG3-N3 functions as a click-chemistry reagent containing an azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can also react through strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO- or BCN-containing compounds, thereby supporting targeted PROTAC assembly and bioconjugation for chemical biology and drug-discovery applications.

GSH linker-2 is an ADC linker, utilized in the synthesis of GNE-987 GSH linker-2.