GSK 650394
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GSK 650394是一种血清和糖皮质激素调节激酶1(SGK1)的小分子抑制剂,IC50值为13 nM[1].
Sgk1基因是一种雄激素靶基因.敲除SGK1基因表达可减弱雄激素介导的前列腺癌细胞系的生长.因此,抑制SGK1是一种新的前列腺癌治疗机制.GSK 650394是一种SGK1竞争性抑制剂.它对纯化的SGK1显示出有效的抑制活性,在荧光偏振检测实验中IC50值为13 nM.在基于活性的闪烁迫近分析法测试中,GSK 650394可以阻止SGK1和SGK2的磷酸化活性,IC50值分别为62 nM和103 nM.而且,GSK 650394抑制LNCaP细胞中雄激素介导的Nedd4-2磷酸化增加.GSK 650394也显著地抑制雄激素刺激的细胞增长,IC50值为1 μM[1].
参考文献:
[1] Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483.
- 1. Rong Li, Xiaoqiu Wang, et al. "The role of epithelial Progesterone Receptor Isoforms in embryo implantation." iScience. 2021 Nov 20;24(12):103487. PMID:34934913
- 2. Koesema E, Kodadek T. "Global analysis of gene expression mediated by OX1 orexin receptor signaling in a hypothalamic cell line." PLoS One. 2017 Nov 16;12(11):e0188082. PMID:29145494
- 3. Dr.Alvaro Diaz. "Condicionamiento de células dendríticas por la capa laminar de Echinococcus granulosus: búsqueda de agonistas y mecanismos a nivel de señalizacón." colibri.udelar.edu.uy.2016.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 382.45 |
Cas No. | 890842-28-1 |
Formula | C25H22N2O2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥19.1 mg/mL in DMSO |
Chemical Name | 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid |
SDF | Download SDF |
Canonical SMILES | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=NC=C(C=C34)C5=CC=CC=C5)C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
激酶实验 [1]: | |
闪烁迫近实验 (SPA) |
在由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以及ATP(终浓度为0.15 mM)组成的缓冲液中,加入PDK1(终浓度为1.1 μg/mL)激活SGK1 S422D(60-431 aa;终浓度为0.275 μg/mL)或SGK2(终浓度为0.875 μg/mL)。在30 °C下,将其孵育30分钟。按SGK1的制备方法制备SGK2,除了SGK2对应其全长蛋白。反应缓冲液包含了生物素化的CROSStide多肽(终浓度为75 μM)和2 × 106 cpm的γ32P-ATP。在96孔板中,将5 μL GSK 650394加入到25 μL激活的酶混合物中。再加入20 μL CROSStide混合物,将其置于室温下培养1小时。加入50 μL 25 mg/mL链霉亲和素包被的SPA磁珠(分散于含0.1 M EDTA,pH 8.0的PBS中)。然后将板密封,以2000 rpm离心8分钟,使用Packard TopCount NXT闪烁计数器,对每个孔检测30秒,收集信号。使用GraphPad Prism 3软件计算GSK650394对SGK1和SGK2的IC50值。 |
细胞实验 [1]: | |
细胞系 |
LNCaP细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
~ 10 μM;7天 |
实验结果 |
在LNCaP细胞中,GSK 650394抑制雄激素介导的Nedd4-2磷酸化增强。此外,GSK 650394也显著抑制雄激素刺激的LNCaP细胞生长,其IC50值约为1 μM。 |
References: [1]. Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483. |
质量控制和MSDS
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