GNE-987 is a highly active chimeric BET degrader that binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low-nanomolar affinity and induces exceptionally potent BRD4 degradation in cells, achieving picomolar DC50 values in EOL-1 acute myeloid leukemia cells, thereby serving as a powerful chemical biology tool for dissecting BET-dependent transcriptional regulation.
Molekulargewicht:
1096.31
CAS Nummer:
[2417371-71-0]
Formel:
C56H67F2N9O8S2
Target-Kategorie:
Epigenetic Reader Domain
T11441
T11441
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