GNE-987

2417371-71-0

1096.31

DMSO : 150 mg/mL (136.82 mM; Need ultrasonic)

Epigenetics; PROTAC

GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC₅₀=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 (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC)^[1]. In Vitro: GNE-987 inhibits EOL-1 and HL-60 cell viability with IC₅₀s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC₅₀ of 0.03 nM^[1].
GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins^[1].