GNE-272 is a potent and highly selective inhibitor of the CBP/EP300 bromodomains. This product inhibits CBP and EP300 with IC50 values of 0.02 µM and 0.03 µM, respectively, exhibiting 650-fold selectivity over BRD4 (IC50 = 13 µM). In cell-based assays, it effectively inhibits MYC expression (EC50 = 0.91 µM) without significant off-target activity against various kinases, receptors, or cytochrome P450 isoforms. As a selective in vivo probe, GNE-272 serves as a vital pharmacological tool for studying CBP/EP300 functions in acute myeloid leukemia (AML) and other cancers.
Molekulargewicht:
424.47
CAS Nummer:
[1936428-93-1]
Formel:
C22H25FN6O2
Target-Kategorie:
Epigenetic Reader Domain
T15400
T15400
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
