EMD638683

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Chemical Structure| 1181770-72-8 同义名 : -
CAS号 : 1181770-72-8
货号 : A759585
分子式 : C18H18F2N2O4
纯度 : 99%+
分子量 : 364.34
MDL号 : MFCD25541743
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 EMD638683 is a selective SGK1 inhibitor. EMD638683 suppresses the phosphorylation of NDRG1 (N-Myc downstream-regulated gene 1), with an IC50 value of 3.35±0.32 μM in the cell culture medium. Additionally, EMD638683 exhibits inhibitory activity against cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), as well as the SGK isoforms SGK2 and SGK3 [1]. In both control and EMD638683 (50 μM)-treated CaCo-2 cells, radiation significantly elevates the proportion of cells undergoing late apoptosis. Treatment with EMD638683 alone tends to increase the percentage of apoptotic CaCo-2 cells. Post-radiation, the proportion of apoptotic EMD638683-treated CaCo-2 cells is notably higher than that of apoptotic control cells. Therefore, EMD638683 treatment substantially enhances apoptosis following radiation [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.45mL

5.49mL

2.74mL
参考文献

[1]Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46.

[2]Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48.

[3]Xi X, et al. Serum-glucocorticoid regulated kinase 1 regulates macrophage recruitment and activation contributing to monocrotaline-induced pulmonary arterial hypertension. Cardiovasc Toxicol. 2014 Dec;14(4):368-78.