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

货号：A324075

GSK 650394是一种 SGK1 和 SGK2 抑制剂，IC50 分别为 62 nM 和 103 nM，能够抑制流感病毒复制，可用于多种疾病研究。

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

货号：A324075 标准纯度： {[allProObj[0].p_purity_real_show]}
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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 细胞实验

Cell Line
Concentration Treated Time Description References
A549 cells 0.78 to 100 µM 24, 48, 72, 96 hours To test the effect of GSK 650394 on the viability of A549 cells. The results showed that cells maintained good viability (≥91%) at 0.78 to 3.13 µM throughout the 96-hour period, at 6.25 to 50 µM up to 48 h (≥75%), and had poor viability (≤64%) at 100 µM. J Virol. 2013 May;87(10):6020-6.

GSK 650394 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Neuropathic pain model Intrathecal injection 100 nM Once daily for 7 days GSK-650394 alleviated neuropathic pain behaviors, reduced pSGK1–kalirin costaining, and attenuated SGK1–kalirin coupling. J Neurosci. 2013 Mar 20;33(12):5227-40

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 382.45
SMILES Code O=C(O)C1=CC=C(C2=CNC3=NC=C(C4=CC=CC=C4)C=C32)C=C1C5CCCC5
MDL No. MFCD12828779
别名
运输蓝冰
InChI Key WVSBGSNVCDAMCF-UHFFFAOYSA-N
Pubchem ID 25022668
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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 参考文献 | GSK 650394 实验方案 | GSK 650394 技术信息

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