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Medchemexpress LLC GNE-781 | 1936422-33-1 | 98.5% | 525.59 | 10 MG
Supplier: Medchemexpress LLC HY1086961MG
GNE-781 is an orally active, highly potent, and selective CBP inhibitor with an IC50 of 0.94 nM in a TR-FRET assay. It also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. It has demonstrated antitumor activity in an MOLM-16 AML xenograft model. GNE-781 is a potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) and is highly selective for CBP/P300.
- Orally active
- Highly potent and selective CBP inhibitor
- Inhibits BRET and BRD4(1)
- Displays antitumor activity in an MOLM-16 AML xenograft model
- Reduces FOXP3 (forkhead box P3) transcript levels
- Exquisitely selective for CBP/P300
- Decreases Foxp3 transcript levels in a dose-dependent manner in vivo
- Suppresses MYC in vivo
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