2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸

中文名	GSK 650394
英文名	2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid
别名	SGK抑制剂(GSK 650394) 2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸
英文别名	CS-1142 GSK 650394 GSK650394 (Free base) SGK inhibitor GS650394 6-O-α-D-Glucopyranosyl-D-glucose 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid Benzoic acid, 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-
CAS	890842-28-1
化学式	C25H22N2O2
分子量	382.45
溶解度	DMSO: 可溶20mg/mL，澄清
存储条件	room temp
外观	粉末
颜色	white to beige
靶点	IC50: 62 nM (SGK1), 103 nM (SGK2)
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。
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.
WGK Germany	3
参考资料展开查看	1: Su Y, Qadri SM, Cayabyab FS, Wu L, Liu L. Regulation of methylglyoxal-elicited leukocyte recruitment by endothelial SGK1/GSK3 signaling. Biochim Biophys Acta. 2014 Jul 5;1843(11):2481-2491. doi: 10.1016/j.bbamcr.2014.06.018. [Epub ahead of print] PubMed PMID: 25003317. 2: Zhang L, Liu J, Liu Y, Xu Y, Zhao X, Qian J, Sun B, Xing C. Fluvastatin inhibits the expression of fibronectin in human peritoneal mesothelial cells induced by high-glucose peritoneal dialysis solution via SGK1 pathway. Clin Exp Nephrol. 2014 Jun 20. [Epub ahead of print] PubMed PMID: 24942605. 3: Mattes C, Laube M, Thome UH. Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells. Physiol Rep. 2014 Mar 20;2(3):e00269. doi: 10.1002/phy2.269. Print 2014. PubMed PMID: 24760523; PubMed Central PMCID: PMC4002249. 4: Isikbay M, Otto K, Kregel S, Kach J, Cai Y, Vander Griend DJ, Conzen SD, Szmulewitz RZ. Glucocorticoid receptor activity contributes to resistance to androgen-targeted therapy in prostate cancer. Horm Cancer. 2014 Apr;5(2):72-89. doi: 10.1007/s12672-014-0173-2. Epub 2014 Mar 11. PubMed PMID: 24615402. 5: Chatterjee S, Schmidt S, Pouli S, Honisch S, Alkahtani S, Stournaras C, Lang F. Membrane androgen receptor sensitive Na+/H+ exchanger activity in prostate cancer cells. FEBS Lett. 2014 May 2;588(9):1571-9. doi: 10.1016/j.febslet.2014.02.040. Epub 2014 Mar 4. PubMed PMID: 24607544. 6: Bradford D, Raghuram V, Wilson JL, Chou CL, Hoffert JD, Knepper MA, Pisitkun T. Use of LC-M

2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸 - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	2.615 ml	13.074 ml	26.147 ml
5 mM	0.523 ml	2.615 ml	5.229 ml
10 mM	0.261 ml	1.307 ml	2.615 ml
5 mM	0.052 ml	0.261 ml	0.523 ml

最后更新：2024-01-02 23:10:35

2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸 - 细胞实验

LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer’s instructions.(Only for Reference) Cell lines: LNCaP cells

最后更新：2023-08-16 21:32:38

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CAS: 890842-28-1
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湖北扬信医药科技有限公司

产品名: GSK 650394 询盘
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CAS: 890842-28-1
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产品描述: 中文名：2-环戊基-4-(5-苯基-1H-吡咯并[2,3-b]吡啶-3-基)苯甲酸英文名:GSK650394 CAS:890842-28-1 规格:98% 产更多

上海麦克林生化科技股份有限公司

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产品名: GSK650394 去供应商网站查看询盘
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上海源叶生物科技有限公司

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