EMD638683

• CAT Number: I000645
• CAS Number: 1181770-72-8
• Molecular Formula: C18H18F2N2O4
• Molecular Weight: 364.34
• Purity: ≥95%
• Synonyms: N/’-[2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide
• Target: SGK
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 3 uM
• InChI: 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)
• InChIKey: SSNAPUUWBPZGOY-UHFFFAOYSA-N
• SMILES: O=C(NNC(C(C1=CC(F)=CC(F)=C1)O)=O)C2=CC=C(O)C(C)=C2CC

EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 uM.IC50 Value: 3 uMTarget: SGK1The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drugs counteracting hypertension in individuals with type II diabetes and metabolic syndrome.in vitro: EMD638683 was tested in vitro by determination of SGK1-dependent phosphorylation of NDRG1 (N-Myc downstream-regulated gene 1) in human cervical carcinoma HeLa-cells. EMD638683 was a SGK1 inhibitor with an IC50 of 3 μM[1].in vivo: 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[1].

Reference

1:Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Towhid ST, Liu GL, Ackermann TF, Beier N, Scholz W, Fuchß T, Toulany M, Rodemann HP, Lang F.Cell Physiol Biochem. 2013;32(4):838-48. doi: 10.1159/000354486. Epub 2013 Sep 20. PMID: 24081014 Free Article2:EMD638683, a novel SGK inhibitor with antihypertensive potency. Ackermann TF, Boini KM, Beier N, Scholz W, Fuchss T, Lang F.Cell Physiol Biochem. 2011;28(1):137-46. doi: 10.1159/000331722. Epub 2011 Aug 16. PMID: 21865856 Free Article