GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 . 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 nano
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
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Product Description
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 . 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 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)
In Vitro
GNE-987 inhibits EOL-1 and HL-60 cell viability with IC 50 s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC 50 of 0.03 nM. GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: EOL-1 cells Concentration: 0.1, 1, 10 nM Incubation Time: 5 hours Result: Degraded the BRD2 and BRD3 BET family proteins.
This compound belongs to the class of organic compounds known as dipeptides. These are organic compounds containing a sequence of exactly two alpha-amino acids joined by a peptide bond.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
