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- CAS号：
890842-28-1
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥553.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥242.0 |
| 规格： | 2mg | 产品价格： | ￥321.0 |
| 规格： | 5mg | 产品价格： | ￥504.0 |
| 规格： | 10mg | 产品价格： | ￥757.0 |
| 规格： | 25mg | 产品价格： | ￥1456.0 |
| 规格： | 50mg | 产品价格： | ￥2224.0 |
| 规格： | 100mg | 产品价格： | ￥3032.0 |
| 规格： | 200mg | 产品价格： | ￥4344.0 |
Product Introduction
Bioactivity
| 名称 | GSK 650394 |
| 描述 | GSK 650394 is an inhibitor of serum- and glucocorticoid-regulated kinases (SGK) that inhibits SGK1 and SGK2 (IC50=62/103 nM). GSK 650394 has antitumor activity and also inhibits osteoclast differentiation and prevents bone loss. |
| 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) |
| 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. |
| 体外活性 | 方法：LNCaP 细胞用 GSK 650394 (0.1-10 µM) 和 R1881 (1 nM) 处理 24-48 h，通过 Western Blot 检测靶点蛋白表达水平。 结果：GSK 650394 抑制了雄激素介导的 Nedd4-2 磷酸化增强，表明 GSK 650394 拮抗了细胞中的 SGK1 活性。[1] 方法：肿瘤细胞 HeLa 和 HepG2 用 GSK 650394 (3.12-12.5 µM) 处理 24-72 h，通过 MTT assay 测定细胞活力。 结果：用 GSK 650394 处理的细胞以剂量依赖的方式显示出显著的生长抑制作用。[2] |
| 体内活性 | 方法：为研究对骨质疏松症的作用，将 GSK 650394 (10-30 mg/kg) 腹腔注射给卵巢切除诱导的骨丢失小鼠，每周三次，持续八周。 结果：GSK 650394 治疗改善了卵巢切除诱导的骨丢失小鼠的骨密度。GSK 650394 治疗可以提高体内抗氧化酶的能力。研究表明，GSK 650394 可以抑制破骨细胞的活化，因此可能是治疗破骨细胞活化相关骨质疏松症的潜在治疗试剂。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Corn oil : < 10 mg/mL (26.15 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 10 mg/mL (26.15 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% Corn Oil : 2.5 mg/mL (6.54 mM), Sonication is recommended. 10% DMSO+90% Saline : < 10 mg/mL (26.15 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 50 mg/mL (130.74 mM), Sonication is recommended. 10% DMSO+90% (20% SBE-β-CD in Saline) : < 10 mg/mL (26.15 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | SGK2 | SGK1 | SGK | Serum-glucocorticoid regulated kinase | Serum and glucocorticoid-regulated kinase | Inhibitor | inhibit | InfluenzaVirus | Influenza Virus | GSK-650394 | GSK 650394 |
| 相关产品 | Baicalein | Salcomine | β-Cyclodextrin | Nitazoxanide | Curcumin | Dihydromyricetin | α-Vitamin E | Acetylcysteine | Naringenin | Benzimidazole | Rifampicin | Molnupiravir |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Metabolism Compound Library | Anti-Infection Compound Library | Kinase Inhibitor Library | NO PAINS Compound Library | Anti-Viral Compound Library | Glycometabolism Compound Library | Anti-Metabolism Disease Compound Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 GSK650394【890842-28-1】
￥242 - 4344
