2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸
- CAS号:890842-28-1
- 英文名:2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid
- 中文名:2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸
- CBNumber:CB52518968
- 分子式:C25H22N2O2
- 分子量:382.45
- MOL File:890842-28-1.mol
- 储存条件 :room temp
- 溶解度 :DMSO: soluble20mg/mL, clear
- 形态 :powder
- 颜色 :white to beige
- WGK Germany :3
2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸性质、用途与生产工艺
- 生物活性 GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。
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靶点
Target Value SGK1
(Cell-free assay)62 nM SGK2
(Cell-free assay)103 nM -
体外研究
GSK650394抑制SGK1介导的上皮细胞转运,在SCC试验中IC50为0.6 μM。在LNCaP细胞中,GSK650394抑制雄激素介导的Nedd4-2磷酸化增加和雄激素介导的细胞生长。 GSK650394抵消皮质醇诱导的神经再生的减少,Hedgehog信号通路的改变,和GR核转运。GSK 650394通过减弱流感vRNPs转运到A549细胞的细胞质抑制流感病毒的复制。
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体内研究
GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevents CFA-induced pain behavior and the associates SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration. GSK650394 at concentrations of 10, 30, and 100 nM (10 μL), but not vehicle solution (SNL 3D+Veh and SNL 7D+Veh, respectively), dose-dependently increases the withdrawal latency of the ipsilateral hindpaw at 1-3 and 1-5 h after injection at days 3 and 7 postsurgery (SNL 3D+GSK and SNL 7D+GSK, respectively). GSK650394 (from day 0 to 6 postsurgery; 100 nM, 10 μL, i.t.) administration alleviates SNL-induced allodynia at days 3, 5, and 7 postsurgery in SNL animals.
- 更新日期:2024/11/08
- 产品编号:HY-15192
- 产品名称:GSK 650394
- CAS编号:
- 包装:1 mg
- 价格:363元
- 更新日期:2024/11/08
- 产品编号:S7209
- 产品名称:2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸 GSK650394
- CAS编号:890842-28-1
- 包装:5mg
- 价格:806.76元
- 公司名称:Novachemistry
- 联系电话:44-20819178-90 02081917890
- 电子邮件:info@novachemistry.com
- 国家:英国
- 产品数:4381
- 优势度:58
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77