EMD638683
- Product Name
- EMD638683
- CAS No.
- 1181770-72-8
- Chemical Name
- EMD638683
- Synonyms
- ]-2-ethyL;EMD638683;N'-[2-(3,5-DifL;)-2-hydroxyacetyL;-4-hydroxy-3-methyL;EMD 638683;EMD-638683;EMD638683, 10 mM in DMSO;N'-(2-(3,5-difluorophenyl)-2-hydroxyacetyl)-2-ethyl-4-hydroxy-3-methylbenzohydrazide;2-(3,5-difluorophenyl)-N'-(2-ethyl-4-hydroxy-3-met hylbenzoyl)-2-hydroxyacetohydrazide;Benzeneacetic acid, 3,5-difluoro-α-hydroxy-, 2-(2-ethyl-4-hydroxy-3-methylbenzoyl)hydrazide
- CBNumber
- CB92627800
- Molecular Formula
- C18H18F2N2O4
- Formula Weight
- 364.34
- MOL File
- 1181770-72-8.mol
EMD638683 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML3410
- Product name
- EMD638683
- Purity
- ≥98% (HPLC)
- Packaging
- 10 mg
- Price
- $272.65
- Updated
- 2025/07/31
- Product number
- SML3410
- Product name
- EMD638683
- Purity
- ≥98% (HPLC)
- Packaging
- 50 mg
- Price
- $1150
- Updated
- 2025/07/31
- Product number
- CS-1344
- Product name
- EMD638683
- Purity
- 99.74%
- Packaging
- 100mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- CS-1344
- Product name
- EMD638683
- Purity
- 99.74%
- Packaging
- 5mg
- Price
- $312
- Updated
- 2021/12/16
- Product number
- A3389
- Product name
- EMD638683
- Packaging
- 10mg
- Price
- $336
- Updated
- 2021/12/16
EMD638683 Chemical Properties,Usage,Production
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
EMD638683 Preparation Products And Raw materials
Raw materials
Preparation Products
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