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GSK650394
GSK650394是一種血清和糖皮質(zhì)激素調(diào)節(jié)的激酶-1抑制劑,對SGK1和SGK2的 IC50分別為62 nM和103 nM。
GSK650394 Chemical Structure
CAS: 890842-28-1
產(chǎn)品質(zhì)控
批次：
純度：
99.92%
99.92
GSK650394相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | SGK1 SGK2 SGK3 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | PROTAC SGK3 degrader-1 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點(diǎn)擊展開 |
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | GSK650394是一種血清和糖皮質(zhì)激素調(diào)節(jié)的激酶-1抑制劑,對SGK1和SGK2的 IC50分別為62 nM和103 nM。 | ||||
|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | GSK650394抑制SGK1介導(dǎo)的上皮細(xì)胞轉(zhuǎn)運(yùn)，在SCC試驗(yàn)中IC50為0.6 μM。在LNCaP細(xì)胞中，GSK650394抑制雄激素介導(dǎo)的Nedd4-2磷酸化增加和雄激素介導(dǎo)的細(xì)胞生長。[2] GSK650394抵消皮質(zhì)醇誘導(dǎo)的神經(jīng)再生的減少，Hedgehog信號通路的改變，和GR核轉(zhuǎn)運(yùn)。GSK 650394通過減弱流感vRNPs轉(zhuǎn)運(yùn)到A549細(xì)胞的細(xì)胞質(zhì)抑制流感病毒的復(fù)制。[3] | |||
|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 閃爍迫近分析法 (SPA) | |||
| SGK1 S422D(60–431 aa；0.275 μg/mL 終濃度)或SGK2 (0.875 μg/mL終濃度)在緩沖液中被PDK1 (1.1 μg/mL終濃度)激活，在30℃下培養(yǎng)30分鐘，緩沖液由50 mM Tris (pH 7.5)，0.1 mM EGTA，0.1 mM EDTA，10 mM MgCl2，0.1% β-巰基乙醇， 1 mg/mL BSA，和ATP (終濃度0.15 mM)組成。SGK2的制備如SGK1，除了其對應(yīng)的全長蛋白質(zhì)。包含終濃度為75 μM的生物素化的CROSStide多肽溶液和2×106 cpm的γ32P-ATP在反應(yīng)緩沖液中制備。在96孔板中，將5 μL GSK650394加入25 μL激活的酶混合物。加入20 μL CROSStide混合物，并在室溫下培養(yǎng)1小時(shí)。接下來，加入含0.1 M EDTA，pH 8.0的50 μL 25 mg/mL鏈霉親和素包被的SPA珠PBS懸浮液。然后將板密封，以2000 rpm離心8分鐘，信號以30 sec/well在Packard TopCount NXT 閃爍計(jì)數(shù)器上檢測。GSK650394抑制SGK1 和 SGK2 活性的IC50值通過這些數(shù)據(jù)使用GraphPad Prism 3軟件計(jì)算。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | LNCaP 細(xì)胞 | ||
| 濃度 | ~10 μM | |||
| 孵育時(shí)間 | 7天 | |||
| 方法 | LNCaP細(xì)胞以5,000細(xì)胞每孔的密度接種于96孔板，在100 μL PRF-RPMI 1640中培養(yǎng)，用8% CS-FBS，0.1 mM NEAA，和1 mM NaPyr進(jìn)行補(bǔ)充。在第三天，通過50 μL PRF-RPMI 1640 取代原培養(yǎng)基，其包含8% CS-FBS，NEAA，NaPyr 和2X 濃度的適當(dāng)激素/抑制劑，細(xì)胞被含有或不含有GSK650394的激素處理。在第5天和第7天，重復(fù)處理。在第10天，除去培養(yǎng)基，相對細(xì)胞數(shù)通過FluoReporter Blue試驗(yàn)根據(jù)制造商說明進(jìn)行測定。 | |||
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | 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 | |
化學(xué)信息&溶解度
| 分子量 | 382.45 | 分子式 | C25H22N2O2 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 76 mg/mL ( (198.71 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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