GSK650394
GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。
GSK650394 Chemical Structure
CAS: 890842-28-1
产品质控
批次：
纯度：
99.92%
99.92
GSK650394相关产品
| 相关靶点 | SGK1 SGK2 SGK3 | 点击展开 |
|---|---|---|
| 相关产品 | PROTAC SGK3 degrader-1 | 点击展开 |
| 相关化合物库 | 代谢化合物库 抗癌代谢化合物库 谷氨酰胺代谢化合物库 糖代谢化合物库 脂代谢化合物库 | 点击展开 |
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human M-1 cells | Function assay | Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment, IC50=0.58 μM | 19497745 | ||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.1649 μM | SANGER | ||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.51532 μM | SANGER | ||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=0.78455 μM | SANGER | ||
| human KM12 cell | Growth inhibition assay | Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.85069 μM | SANGER | ||
| human GDM-1 cell | Growth inhibition assay | Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.87937 μM | SANGER | ||
| human RT-112 cell | Growth inhibition assay | Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.02782 μM | SANGER | ||
| human MONO-MAC-6 cell | Growth inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=1.18097 μM | SANGER | ||
| human HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.30172 μM | SANGER | ||
| human HGC-27 cell | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=1.30821 μM | SANGER | ||
| human LCLC-97TM1 cell | Growth inhibition assay | Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=1.36768 μM | SANGER | ||
| human LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.40152 μM | SANGER | ||
| human HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=1.42683 μM | SANGER | ||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=1.57869 μM | SANGER | ||
| human SNG-M cell | Growth inhibition assay | Inhibition of human SNG-M cell growth in a cell viability assay, IC50=1.79853 μM | SANGER | ||
| human MCF7 cell | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=1.8178 μM | SANGER | ||
| human A431 cell | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50=1.85902 μM | SANGER | ||
| human BC-3 cell | Growth inhibition assay | Inhibition of human BC-3 cell growth in a cell viability assay, IC50=1.87094 μM | SANGER | ||
| human A427 cell | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=1.87611 μM | SANGER | ||
| human SW620 cell | Growth inhibition assay | Inhibition of human SW620 cell growth in a cell viability assay, IC50=1.92816 μM | SANGER | ||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50=1.97312 μM | SANGER | ||
| human MFH-ino cell | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=1.98658 μM | SANGER | ||
| human TE-12 cell | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.99128 μM | SANGER | ||
| human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.1871 μM | SANGER | ||
| human NCI-H2342 cell | Growth inhibition assay | Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=2.19053 μM | SANGER | ||
| human BC-1 cell | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay, IC50=2.51651 μM | SANGER | ||
| human TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=2.59181 μM | SANGER | ||
| human T84 cell | Growth inhibition assay | Inhibition of human T84 cell growth in a cell viability assay, IC50=2.60446 μM | SANGER | ||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.70082 μM | SANGER | ||
| human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=2.71158 μM | SANGER | ||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.76731 μM | SANGER | ||
| human OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=2.78861 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 EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=3.01558 μM | SANGER | ||
| human 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM | SANGER | ||
| human PA-1 cell | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.33083 μM | SANGER | ||
| human NCI-H2122 cell | Growth inhibition assay | Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=3.333 μM | SANGER | ||
| human NCI-H460 cell | Growth inhibition assay | Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=3.4041 μM | SANGER | ||
| human CHL-1 cell | Growth inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=3.49665 μM | SANGER | ||
| human MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.51555 μM | SANGER | ||
| human HCT-15 cell | Growth inhibition assay | Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=3.62842 μM | SANGER | ||
| human G-361 cell | Growth inhibition assay | Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.71745 μM | SANGER | ||
| human SK-LU-1 cell | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.97014 μM | SANGER | ||
| human ES4 cell | Growth inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay, IC50=4.06069 μM | SANGER | ||
| human TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.11582 μM | SANGER | ||
| human IGR-1 cell | Growth inhibition assay | Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=4.233 μM | SANGER | ||
| human SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=4.46124 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 CAL-27 cell | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=5.33221 μM | SANGER | ||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=5.35583 μM | SANGER | ||
| human SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=5.38255 μM | SANGER | ||
| human HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=5.49347 μM | SANGER | ||
| human NCI-H1299 cell | Growth inhibition assay | Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.98557 μM | SANGER | ||
| human HT-29 cell | Growth inhibition assay | Inhibition of human HT-29 cell growth in a cell viability assay, IC50=7.26843 μM | SANGER | ||
| human A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM | SANGER | ||
| human SK-MEL-30 cell | Growth inhibition assay | Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=7.97215 μM | SANGER | ||
| human CMK cell | Growth inhibition assay | Inhibition of human CMK cell growth in a cell viability assay, IC50=8.25377 μM | SANGER | ||
| human HuP-T4 cell | Growth inhibition assay | Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=8.50234 μM | SANGER | ||
| human SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=8.80208 μM | SANGER | ||
| human MKN1 cell | Growth inhibition assay | Inhibition of human MKN1 cell growth in a cell viability assay, IC50=9.18565 μM | SANGER | ||
| human LoVo cell | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50=9.91292 μM | SANGER | ||
| human HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50=10.68 μM | SANGER | ||
| human SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=13.6896 μM | SANGER | ||
| human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=13.7916 μM | SANGER | ||
| human HuH-7 cell | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=18.2783 μM | SANGER | ||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=20.4955 μM | SANGER | ||
| human MC116 cell | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay, IC50=21.2676 μM | SANGER | ||
| human H4 cell | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50=21.4244 μM | SANGER | ||
| human SK-MEL-3 cell | Growth inhibition assay | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=30.0228 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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。[2] 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。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 闪烁迫近分析法 (SPA) | |||
| SGK1 S422D(60–431 aa；0.275 μg/mL 终浓度)或SGK2 (0.875 μg/mL终浓度)在缓冲液中被PDK1 (1.1 μg/mL终浓度)激活，在30℃下培养30分钟，缓冲液由50 mM Tris (pH 7.5)，0.1 mM EGTA，0.1 mM EDTA，10 mM MgCl2，0.1% β-巯基乙醇， 1 mg/mL BSA，和ATP (终浓度0.15 mM)组成。SGK2的制备如SGK1，除了其对应的全长蛋白质。包含终浓度为75 μM的生物素化的CROSStide多肽溶液和2×106 cpm的γ32P-ATP在反应缓冲液中制备。在96孔板中，将5 μL GSK650394加入25 μL激活的酶混合物。加入20 μL CROSStide混合物，并在室温下培养1小时。接下来，加入含0.1 M EDTA，pH 8.0的50 μL 25 mg/mL链霉亲和素包被的SPA珠PBS悬浮液。然后将板密封，以2000 rpm离心8分钟，信号以30 sec/well在Packard TopCount NXT 闪烁计数器上检测。GSK650394抑制SGK1 和 SGK2 活性的IC50值通过这些数据使用GraphPad Prism 3软件计算。 | ||||
| 细胞实验 | 细胞系 | LNCaP 细胞 | ||
| 浓度 | ~10 μM | |||
| 孵育时间 | 7天 | |||
| 方法 | LNCaP细胞以5,000细胞每孔的密度接种于96孔板，在100 μL PRF-RPMI 1640中培养，用8% CS-FBS，0.1 mM NEAA，和1 mM NaPyr进行补充。在第三天，通过50 μL PRF-RPMI 1640 取代原培养基，其包含8% CS-FBS，NEAA，NaPyr 和2X 浓度的适当激素/抑制剂，细胞被含有或不含有GSK650394的激素处理。在第5天和第7天，重复处理。在第10天，除去培养基，相对细胞数通过FluoReporter Blue试验根据制造商说明进行测定。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-SGK2 / SGK2 p-SGK1 / SGK1 c-Jun / NRF2 p21 / LC3 / p62 / PARP / Cleaved PARP |
|
26392083 | |
| Immunofluorescence | LC3 |
|
29017179 | |
| Growth inhibition assay | Cell viability |
|
29017179 | |
化学信息&溶解度
| 分子量 | 382.45 | 分子式 | C25H22N2O2 |
| CAS号 | 890842-28-1 | SDF | Download GSK650394 SDF |
| Smiles | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 76 mg/mL ( (198.71 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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