GNE-781 (compound 19) is a highly potent, orally active, selective bromodomain inhibitor against cyclic adenosine monophosphate response element binding protein (CBP). The IC50 value is 0.94 nM (in TR-FRET assay). GNE-781 also suppresses BRET and BRD4(1), with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 has antitumor activity.
Molekulargewicht:
525.59
Reinheit:
>99%
CAS Nummer:
[1936422-33-1]
Formel:
C27H33F2N7O2
Target-Kategorie:
Epigenetic Reader Domain
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