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GSK2801

CAS No. : 1619994-68-1

MCE 站：GSK2801

产品活性：GSK2801 是一种有效的，选择性的，口服活性的和细胞活性的乙酰赖氨酸竞争性 BAZ2A 和 BAZ2B 溴结构域抑制剂，K_d 值分别为 136 nM 和 257 nM。GSK2801 对 BAZ2A/B 的选择性是 BRD4 的 50 倍以上。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

In Vitro: GSK2801 binds TAF1L(2) with an affinity K_B of 0.31μM (K_D: 3.2 μM) and a binding enthalpy change ΔH of ?8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K_B of 0.826 μM (K_D: 1.1 μM) and ΔH of ?9.8 kcal/mol.
GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC.

In Vivo: In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.

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