GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. 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].
Molecular Weight:
1096.31
Purity:
99.98
CAS Number:
[2417371-71-0]
Formula:
C56H67F2N9O8S2
Target:
Epigenetic Reader Domain,PROTACs
Application Notes:
MCE Product type: Reference compound
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