GSK2801
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- CAS号:
- 1619994-68-1
- 英文名:
- GSK 2801
- 英文别名:
- GSK 280;CS-1607;GSK2801;GSK-2801;GSK 2801;GSK2801, >98%;GSK-2801; GSK 280;GSK2801 GSK-2801;GSK2801;GSK-2801;GSK 2801;1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
- 中文名:
- GSK2801
- 中文别名:
- 化合物GSK2801;GSK2801,BAZ2A和BAZ2B抑制剂;BAZ2A和BAZ2B抑制剂(GSK2801);1-(1-(2-(甲磺酰)苯基)-7-丙氧基吲哚嗪-3-基)乙酮;1-[1-[2-(甲基磺酰基)苯基]-7-丙氧基-3-吲哚嗪基]乙酮
- CBNumber:
- CB52668513
- 分子式:
- C20H21NO4S
- 分子量:
- 371.45
- MOL File:
- 1619994-68-1.mol
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GSK2801化学性质
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密度:
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1.23±0.1 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥2.82 mg/mL in EtOH with gentle warming and ultrasonic
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形态:
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solid
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GSK2801性质、用途与生产工艺
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，Kd 值分别为 136 nM 和 257 nM。GSK2801 对 BAZ2A/B 的选择性是 BRD4 的 50 倍以上。
Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B)
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 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.
GSK2801
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-15658 | GSK2801 | | 1 mg | 260元 |
| 2024/01/25 | HY-15658 | GSK2801
GSK2801 | 1619994-68-1 | 5mg | 650元 |
1619994-68-1, GSK2801 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- GSK2801,BAZ2A和BAZ2B抑制剂
- 化合物GSK2801
- 1-(1-(2-(甲磺酰)苯基)-7-丙氧基吲哚嗪-3-基)乙酮
- BAZ2A和BAZ2B抑制剂(GSK2801)
- 1-[1-[2-(甲基磺酰基)苯基]-7-丙氧基-3-吲哚嗪基]乙酮
- 1619994-68-1
- inhibit,Inhibitor,GSK-2801,TNBC,BAZ2A,GSK2801,Epigenetic Reader Domain,Apoptosis,BAZ2B,cetyl-lysine,orally,GSK 2801
- GSK2801 GSK-2801
- 1-[1-(2-Methanesulfonyl-phenyl)-7-propoxy-indolizin-3-yl]-ethanone
- GSK2801;GSK-2801;GSK 2801
- CS-1607
- GSK2801, >98%
- GSK 280
- GSK-2801; GSK 280
- Ethanone, 1-[1-[2-(methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]-
- 1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
- 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone
- 1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone
- GSK-2801
- GSK2801
- GSK 2801