GSK 650394
产品说明书
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同义名 : | - |
| CAS号 : | 890842-28-1 | |
| 货号 : | A324075 | |
| 分子式 : | C25H22N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 382.454 | |
| MDL号 : | MFCD12828779 | |
| 存储条件： |
Pure form Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 40 mg/mL(104.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | SGK1 (glucocorticoid-regulated kinase 1) belongs to the AGC family of serine/threonine protein kinases. SGK1 expression is regulated by glucocorticoids and serum, in addition to various other types of signals. SGK1 has been implicated in the regulation of cell growth and survival downstream of PI3K activation. GSK650394 inhibites the enzymatic activity of SGK1 and SGK2 in the SPA assay with IC50 values of 62 nM and 103 nM, respectively. GSK650394 is relatively non-toxic, with LC50 values of 41 μM in M1 cells and a LC50 greater than 100 μM in HeLa cells in XTT assays. Moreover, GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In the LNCaP growth assay, the IC50 of GSK650394 was approximately 1 μM. Furthermore, 10 μM of GSK650394 completely abrogated androgen-mediated growth, indicating that GSK650394 may be an effective approach for the treatment of AR (androgen receptor)-driven prostate cancer [3]. GSK-650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevented CFA (complete Freund's adjuvant)-induced pain behavior and the associated SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration [4]. Daily GSK-650394 administration (from day 0 to 6 postsurgery; 100 nm, 10 μl, i.t.) alleviated SNL-induced allodynia at days 3, 5, and 7 postsurgery compared with animals that received no injection [5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| human 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 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 A375 cell | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.07mL 2.61mL 1.31mL |
26.15mL 5.23mL 2.61mL |
| 参考文献 |
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