GSK-2801
| CAS No. | 1619994-68-1 | Cat. No. | BCP15117 |
| Name | GSK-2801 | ||
| Synonyms | GSK2801;GSK 2801; | ||
| Formula | C20H21NO4S | M. Wt | 371.45 |
| Description | GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology. | ||
| Pathways | Epigenetics | ||
| Targets | Epigenetic Reader Domain | ||
Structure
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