产品信息
抗原名称
SGK
商品描述
EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.
分子量
364.34
纯度
≥98%
可溶性
DMSO : ≥ 50 mg/mL (137.23 mM)
In vitro(体外研究)
EMD638683 is a SGK1 inhibitor. EMD638683 inhibits the NDRG1 (N-Myc downstream-regulated gene 1) phosphorylation, an effect requiring 3.35±0.32 μM EMD638683 in the cell culture medium for half maximal effect (IC50). EMD638683 has also an inhibitory effect on cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), and the SGK isoforms SGK2 and SGK3. In both, control and EMD638683 (50 µM)-treated CaCo-2 cells, radiation significantly increases the percentage of CaCo-2 cells undergoing late apoptosis. EMD638683 treatment alone tends to enhance the percentage of apoptotic CaCo-2 cells. Following radiation the percentage of apoptotic EMD638683-treated CaCo-2 cells is significantly higher than the percentage of apoptotic control cells. Thus, EMD638683 treatment significantly augments the apoptosis following radiation.
In vivo(体内研究)
The colon is significantly longer and the colon weight significantly lower in EMD638683-treated mice than in placebo-treated mice, a finding pointing to an influence of EMD638683 on tumor growth following chemical carcinogenesis. In addition, the stomach weight is significantly lower in the EMD treated group. Most importantly, the number of developing tumors following carcinogenic treatment is significantly blunted by EMD638683 treatment. EMD638683 (20 mg/kg, intragastrically) prevents progression of monocrotaline (MCT)-induced pulmonary vascular remodeling in rats. Hemodynamic characteristics show that EMD638683 treatment attenuates right ventricular systolic pressure (RVSP) (15.8±2.5 vs. 28.2±3.1 mmHg; P.
背景
别名
EMD 638683；EMD-638683
分子式
C18H18F2N2O4
CAS号
1181770-72-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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