GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research.
GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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