GSK2801 是一种有口服活性的和细胞活性的乙酰赖氨酸竞争性BAZ2A和BAZ2B溴结构域选择性抑制剂，Kd值分别为 136 nM 和 257 nM。

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin. [1]

In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. [1]

1619994-68-1

C20H21NO4S

371.45

DMSO:18.6 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years