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GSK 650394 {[allProObj[0].p_purity_real_show]}

货号：A324075

GSK650394 inhibits the activities of SGK1 and SGK2 with IC50 of 62 nM and 103 nM, respectively.

GSK 650394 化学结构 CAS号：890842-28-1
GSK 650394 化学结构
CAS号：890842-28-1
GSK 650394 3D分子结构
CAS号：890842-28-1
GSK 650394 化学结构 CAS号：890842-28-1
GSK 650394 3D分子结构 CAS号：890842-28-1
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GSK 650394 纯度/质量文件 产品仅供科研

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GSK 650394 生物活性

描述 SGK1 (glucocorticoid-regulated kinase 1) belongs to the AGC family of serine/threonine protein kinases. SGK1 expression is regulated by glucocorticoids and serum, in addition to various other types of signals. SGK1 has been implicated in the regulation of cell growth and survival downstream of PI3K activation. GSK650394 inhibites the enzymatic activity of SGK1 and SGK2 in the SPA assay with IC50 values of 62 nM and 103 nM, respectively. GSK650394 is relatively non-toxic, with LC50 values of 41 μM in M1 cells and a LC50 greater than 100 μM in HeLa cells in XTT assays. Moreover, GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In the LNCaP growth assay, the IC50 of GSK650394 was approximately 1 μM. Furthermore, 10 μM of GSK650394 completely abrogated androgen-mediated growth, indicating that GSK650394 may be an effective approach for the treatment of AR (androgen receptor)-driven prostate cancer [3]. GSK-650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevented CFA (complete Freund's adjuvant)-induced pain behavior and the associated SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration [4]. Daily GSK-650394 administration (from day 0 to 6 postsurgery; 100 nm, 10 μl, i.t.) alleviated SNL-induced allodynia at days 3, 5, and 7 postsurgery compared with animals that received no injection [5].

GSK 650394 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM SANGER
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=2.94825 μM SANGER
human A375 cell Growth inhibition assay Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM SANGER
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM SANGER

GSK 650394 参考文献

[1]Anacker C, Cattaneo A, et al. Role for the kinase SGK1 in stress, depression, and glucocorticoid effects on hippocampal neurogenesis. Proc Natl Acad Sci U S A. 2013 May 21;110(21):8708-13.

[2]Sherk AB, Frigo DE, 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.

[3]Sherk AB, Frigo DE, Schnackenberg CG, Bray JD, Laping NJ, Trizna W, Hammond M, Patterson JR, Thompson SK, Kazmin D, Norris JD, McDonnell DP. 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. doi: 10.1158/0008-5472.CAN-08-1047. PMID: 18794135; PMCID: PMC2562281.

[4]Peng HY, Chen GD, Hsieh MC, Lai CY, Huang YP, Lin TB. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freund's adjuvant-induced inflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012 Dec;153(12):2380-2392. doi: 10.1016/j.pain.2012.08.004. Epub 2012 Sep 11. PMID: 22980744.

[5]Peng HY, Chen GD, Lai CY, Hsieh MC, Lin TB. 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. doi: 10.1523/JNEUROSCI.4452-12.2013. PMID: 23516288; PMCID: PMC6704989.

GSK 650394 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.07mL

2.61mL

1.31mL

26.15mL

5.23mL

2.61mL

GSK 650394 技术信息

CAS号890842-28-1
分子式C25H22N2O2
分子量 382.454
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
溶解度

DMSO: 40 mg/mL(104.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: GSK 650394 | 890842-28-1 | GSK650394 | GSK-650394 | SGK Inhibitor | Metabolic Enzyme/Protease | Anti-infection | SGK | Influenza Virus | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GSK 650394 纯度/质量文件 | GSK 650394 生物活性 | GSK 650394 细胞研究 | GSK 650394 参考文献 | GSK 650394 实验方案 | GSK 650394 技术信息

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