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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
CC1=C(C(C(NNC(C(C2=CC(F)=CC(F)=C2)O)=O)=O)=CC=C1O)CC
InChI
1S/C18H18F2N2O4/c1-3-13-9(2)15(23)5-4-14(13)17(25)21-22-18(26)16(24)10-6-11(19)8-12(20)7-10/h4-8,16,23-24H,3H2,1-2H3,(H,21,25)(H,22,26)
InChI key
SSNAPUUWBPZGOY-UHFFFAOYSA-N
生化/生理作用
EMD638683 is an orally active and highly selective serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC50 = 3 μM against HeLa cellular NDRG1 phosphorylation) that significantly decreased blood pressure in fructose-treated mice but not in control saline-treated or in SGK1-knockout animals (4460 ppm in chow, ~600 mg/kg/day). EMD638683 promotes radiation-induced suicidal death of CaCo-2 colon tumor cells in vitro (50 μM) and decreases the number of colonic tumors following chemical carcinogenesis in vivo (4460 ppm in chow).
Orally active and highly selective serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor with anti-cancer and anti-hypertensive efficacy in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Serum- and glucocorticoid-inducible kinase 1 promotes insulin resistance in adipocytes via degradation of insulin receptor substrate 1
Diabetes & metabolism journal, 37(4), e3451-e3451 (2021)
High-fat diet-induced activation of SGK1 promotes Alzheimer's disease-associated tau pathology
Human Molecular Genetics, 30(18), 1693-1710 (2021)
Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683
Cellular Physiology and Biochemistry, 32(4), 838-848 (2013)
EMD638683, a novel SGK inhibitor with antihypertensive potency
Cellular Physiology and Biochemistry, 28(1), 137-146 (2011)
SGK1.1 limits brain damage after status epilepticus through M current-dependent and independent mechanisms
Neurobiology of Disease, 153, 105317-105317 (2021)
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