GNE-781
| CAS No. | 1936422-33-1 | Cat. No. | BCP29560 |
| Name | GNE-781 | ||
| Synonyms | GNE 781; GNE781; | ||
| Formula | C27H33F2N7O2 | M. Wt | 525.60 |
| Description | GNE-781 is a Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) . GNE-781 showed TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM, BRD4(1) IC50 = 5,100 nΜ) that maintained good in vivo PK properties in multiple species. GNE-781 displays anti-tumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner. | ||
| Pathways | Epigenetics | ||
| Targets | Histone Acetyltransferase Epigenetic Reader Domain | ||
Structure
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