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GSK 650394

GSK 650394

产品编号 T2622   CAS 890842-28-1
别名: GSK650394

GSK 650394 是一种新颖的 SGK 抑制剂,可抑制流感病毒复制。它还是一种血清和糖皮质激素调节的激酶 1 抑制剂。

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GSK 650394 Chemical Structure
GSK 650394, CAS 890842-28-1
规格 价格/CNY 货期 数量
1 mg ¥ 298 现货
2 mg ¥ 423 现货
5 mg ¥ 663 现货
10 mg ¥ 997 现货
25 mg ¥ 1,920 现货
50 mg ¥ 3,190 现货
100 mg ¥ 3,990 现货
200 mg ¥ 5,730 现货
1 mL * 10 mM (in DMSO) ¥ 728 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: GSK 650394 (T2622)
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纯度: 100%
纯度: 98.93%
纯度: 98.34%
纯度: 97.98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK 650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor.
靶点活性 SGK2:103 nM, SGK1:62 nM
体内活性 GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) prevents CFA-induced pain behavior and the associates SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration in a dose-dependent manner[4]. 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[5].
激酶实验 Scintillation proximity assay (SPA): SGK1 S422D (60–431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) are activated by PDK1 (1.1 μg/mL final concentration) in a buffer consisting of 50 mM Tris (pH 7.5), 0.1 mM EGTA, 0.1 mM EDTA, 10 mM MgCl2, 0.1% β-mercaptoethanol, 1 mg/mL BSA, and ATP (final concentration of 0.15 mM) and incubated for 30 min at 30°C. SGK2 is prepared exactly as described for SGK1, except it corresponded to the full-length protein. A solution containing biotinylated CROSStide peptide at a final concentration of 75 μM and γ32P-ATP corresponding to 2×106 cpm is prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK650394 is added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture is added and incubated for 1 h at room temperature. Next, 50 μL of a 25 mg/mL slurry of streptavidin-coated SPA beads in PBS with 0.1 M EDTA, pH 8.0 is added. The plate is then sealed and centrifuged for 8 min at 2000 rpm, and the signal is detected by measuring for 30 sec/well in a Packard TopCount NXT Scintillation Counter. The IC50 values of the inhibition of SGK1 and SGK2 activities by GSK650394 are calculated from these data using GraphPad Prism 3 Software.
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)
别名 GSK650394
分子量 382.45
分子式 C25H22N2O2
CAS No. 890842-28-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 38.2 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6147 mL 13.0736 mL 26.1472 mL 65.368 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL 13.0736 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 mL 6.5368 mL
20 mM 0.1307 mL 0.6537 mL 1.3074 mL 3.2684 mL
50 mM 0.0523 mL 0.2615 mL 0.5229 mL 1.3074 mL
100 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6537 mL

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TargetMol Library Books参考文献

1. Sherk AB, et al. Cancer Res. 2008, 68(18), 7475-7483. 2. Anacker C, et al. Proc Natl Acad Sci U S A. 2013, 110(21), 8708-8713. 3. Alamares-Sapuay JG, et al. J Virol. 2013, 87(10), 6020-6066. 4. Peng HY, et al. 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):2380-92. 5. 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.
SI-113 EMD638683 BRD7389 AT13148 EMD638683 R-Form CKI-7 PROTAC SGK3 degrader-1 URMC-099

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 激酶抑制剂库 经典已知活性库 抗代谢疾病化合物库 抗病毒库 已知活性化合物库 糖代谢化合物库 NO PAINS 化合物库 代谢化合物库 抗感染化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GSK 650394 890842-28-1 Metabolism Microbiology/Virology SGK Influenza Virus inhibit Serum-glucocorticoid regulated kinase Inhibitor GSK650394 Serum and glucocorticoid-regulated kinase GSK-650394 inhibitor

 

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