ChemicalBook CAS DataBase List 1181770-72-8

1181770-72-8

Name	EMD638683
CAS	1181770-72-8
Molecular Formula	C18H18F2N2O4
MDL Number	MFCD25541743
Molecular Weight	364.34
MOL File	1181770-72-8.mol

Chemical Properties

Boiling point	657.6±55.0 °C(Predicted)
density	1.363±0.06 g/cm3(Predicted)
storage temp.	-10 to -25°C
solubility	insoluble in H2O; ≥18.2 mg/mL in DMSO; ≥45.8 mg/mL in EtOH with gentle warming
form	solid
pka	8.68±0.25(Predicted)
color	Off-white to light brown
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	CC1=C(C(C(NNC(C(C2=CC(F)=CC(F)=C2)O)=O)=O)=CC=C1O)CC

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

Uses

EMD638683 is a highly selective SGK1 inhibitor, with an IC50 value of 3 μM.

Biological Activity

EMD638683 is an orally active and highly selective serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC50 = 3 μM against HeLa cellular NDRG1 phosphorylation) th at 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).

in vivo

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^[2]. 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<0.05; n=6) and right ventricular hypertrophy index (RVHI) (0.27±0.02 vs. 0.41±0.06;P<0.05; n=6) compare to vehicle-dosed controls^[3].

target

SGK1

IC 50

SGK1

References

[1] Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46. DOI:10.1159/000331722
[2] Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48. DOI:10.1159/000354486
[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. DOI:10.1007/s12012-014-9260-4
[4] Zhou H, et al. Inhibition of serum- and glucocorticoid-inducible kinase 1 enhances TLR-mediated inflammation and promotes endotoxin-driven organ failure. FASEB J. 2015 Sep;29(9):3737-49. DOI:10.1096/fj.15-270462

Spectrum Detail

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