GNE-987 - CAS 2417371-71-0

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 nM for EOL-1 AML cell line) .

Epigenetic Reader Domain, PROTACs

PROTAC, Chromatin/Epigenetic

2417300

C56H67F2N9O8S2

1096.31

O=C([C@H](C[C@@H](O)C1)N1C([C@@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7

-20°C

Ice Packs

PROTAC