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- 文献和实验
- 技术资料
- 保存条件：
Store at -20℃，6 months.
- 保质期：
Store at -20℃，6 months.
- 英文名：
GSK 650394(10mM in DMSO，Sterile)
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
890842-28-1
- 规格：
1ml
| CAS | 890842-28-1 |
| 英文名称 | GSK 650394(10mM in DMSO，Sterile) |
| 分子式 | C25H22N2O2 |
| 分子量 | 382.45 |
| 规格 | 1ml |
| 溶解性 | 请根据自己的实验要求使用。 |
| 外观(性状) | 无菌溶液 |
| 储存条件 | Store at -20℃，6 months. |
| 运输条件 | 冷冻运输 |
| SMILES | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O |
| InChIKey | WVSBGSNVCDAMCF-UHFFFAOYSA-N |
| InChI | InChI=1S/C25H22N2O2/c28-25(29)20-11-10-18(12-21(20)17-8-4-5-9-17)23-15-27-24-22(23)13-19(14-26-24)16-6-2-1-3-7-16/h1-3，6-7，10-15，17H，4-5，8-9H2，(H，26，27)(H，28，29) |
| PubChem CID | 25022668 |
| 靶点 | SGK |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂。 |
| 生物活性 | GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.[1-5] |
| In Vitro | GSK650394 is relatively non-toxic， with LC50 values of 41 μM in M1 cells (68 times its activity IC50) and a LC50 greater than 100 μM in HeLa cells. GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. GSK650394 inhibits the growth of LNCaP cells with IC50 of approximately 1 μM[1]. GSK650394A inhibits the insulin-induced phosphorylation of PKB-Ser473 at 3 μM， and essentially abolishes this response at 10 μM. GSK650394A (1-10 μM) does not alter the phosphorylation of PRAS40-Ser246 in hormone-deprived cells or prevent the insulin-induced phosphorylation of this residue[2]. |
| In Vivo | 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[3]. 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[4]. |
| 细胞实验 | The toxicity of GSK650394 to M-1 and HeLa cells is assessed using the Cell Proliferation Kit (XTT) following manufacturer’s instructions. Briefly， 10，000 HeLa or M-1 cells/well are plated into 96-well plates in 100μL of the appropriate maintenance media. After 48 h， media is removed and replaced with 100 μL of EMEM with Earle’s salts containing 2 mM L-glutamine and 1% antibiotic-antimycotic overnight. M-1 cells are also supplemented with 1 μg/mL insulin， 6.25 μg/mL sodium selenite， and 6.25 μg/mL transferrin. After 24 h， the media is removed and replaced with 100 μL media alone or media containing increasing concentrations of GSK650394. For HeLa cells， 50 μL of activated XTT solution is added after 4 h. For M-1 cells， 50 μL of activated XTT solution is added after 24 h. Following a 2 h incubation， absorbance is measured at 490 nm using a SpectraMAX PLUS spectrophotometer and the data analyzed to obtain IC50?values using GraphPad Prism 3 software.[1-5] |
| 动物实验 | Briefly， the rats are anesthetized under isoflurane anesthesia (induction 5%， maintenance 2% in oxygen). An incision is made， and the left L5 spinal nerves are carefully isolated and tightly ligated with 6-0 silk sutures 2-5 mm distal to the dorsal root ganglia. GSK650394 (10， 30， and 100 nM， 10 μL) is administered by bolus injection at 3 or 7 d or by daily injection for 7 d (day 0-6) postspinal nerve ligation. A vehicle solution of a volume identical to that of the tested agents is dispensed to serve as a control.[1-5] |
| 数据来源文献 | [1]. Sherk AB， et al. Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008 Sep 15;68(18):7475-83. [2]. Mansley MK， et al. Effects of nominally selective inhibitors of the kinases PI3K， SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. Br J Pharmacol. 2010 Oct;161(3):571-88. [3]. Peng HY， et al. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freunds adjuvant-induced inflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012 Dec;153(12):2380-92. [4]. Peng HY， et al. Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci. 2013 Mar 20;33(12):5227-40. [5]. Alamares-Sapuay JG， et al. Serum- and glucocorticoid-regulated kinase 1 is required for nuclear export of the ribonucleoprotein of influenza A virus. J Virol. 2013 May;87(10):6020-6. |
| 单位 | 瓶 |
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GSK 650394(10mM in DMSO，Sterile)
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