| 名称 | EMD638683 |
| 描述 | EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM). |
| 细胞实验 | Colon carcinoma (Caco-2) cells were exposed to EMD638683 with or without exposure to radiation (3 Gray) and cell volume was estimated from forward scatter, phosphatidylserine exposure from annexin V binding, mitochondrial potential from JC-9 fluorescence, caspase 3 activity from CaspGlow Fluorescein staining, DNA degradation from propidium iodide staining as well as late apoptosis from annexin-V FITC and propidium iodide double staining.?In vivo tumor growth was determined in wild type mice subjected to chemical carcinogenesis (intraperitoneal injection of 20 mg/kg 1,2-dimethylhydrazine followed by three cycles of 30 g/L synthetic dextran sulfate sodium in drinking water for 7 days)[1]. |
| 体外活性 | EMD638683 treatment significantly augmented the radiation-induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis. The in vivo development of tumors following chemical carcinogenesis was significantly blunted by treatment with EMD638683[1]. |
| 体内活性 | Within 24 hours in vivo EMD638683 treatment significantly decreased blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.?EMD638683 failed to alter the blood pressure in SGK1 knockout mice.?Following chronic (4 weeks) fructose/high salt treatment, additional EMD638683 treatment again decreased blood pressure.?EMD638683 thus abrogates the salt sensitivity of blood pressure in hyperinsulinism without appreciably affecting blood pressure in the absence of hyperinsulinism.?EMD638683 tended to increase fluid intake and urinary excretion of Na(+), significantly increased urinary flow rate and significantly decreased body weight[2]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (137.23 mM)
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| 关键字 | inhibit | Serum and glucocorticoid-regulated kinase | Inhibitor | Serum-glucocorticoid regulated kinase | EMD638683 | EMD 638683 | EMD-638683 | SGK |
| 相关产品 | AT13148 | URMC-099 | GSK 650394 | Ro-3306 | EMD638683 R-Form | SGK1-IN-4 | SI-113 | PROTAC SGK3 degrader-1 | CKI-7 | BRD7389 |
| 相关库 | 高选择性抑制剂库 | 糖代谢化合物库 | 经典已知活性库 | 激酶抑制剂库 | 抑制剂库 | NO PAINS 化合物库 | 代谢化合物库 | 已知活性化合物库 | 抗代谢疾病化合物库 |
United States
