GNE 987

GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03

(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, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

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.