EMD638683

Catalog No.S8824 Batch:S882402

Technical Data

Formula	C₁₈H₁₈F₂N₂O₄
Molecular Weight	364.34	CAS No.	1181770-72-8
Solubility (25°C)*	In vitro	DMSO	73 mg/mL (200.36 mM)
		Ethanol	73 mg/mL (200.36 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

EMD638683 is a highly selective inhibitor of serum- and glucocorticoid-inducible kinase 1 (SGK1) with IC50 of 3 μM. EMD638683 exhibits antihypertensive potency and anti-tumor activity.

Targets

SGK1 ^[1]
(Cell-free assay)

3 μM

In vitro

In vitro testing discloses EMD638683 as a SGK1 inhibitor with an IC50 of 3 μM.^[1] EMD638683 treatment significantly augments the radiation‑induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis.^[2]

In vivo

The in vivo development of tumors following chemical carcinogenesis is significantly blunted by treatment with EMD638683.^[2] Within 24 hours in vivo EMD638683 treatment significantly decreases blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HeLa-cells Concentrations 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM Incubation Time 24 h Method The cells are plated in 6-wells MTPs at a density of 10–20 × 10³ cells/cm² in Dulbecco´s DMEM medium, supplemented with 10% fetal calf serum (FCS), 2 mM glutamine and 1 mM sodium pyruvate. After 24 hrs at 37℃ and 5% CO₂ in a cell incubator, each well is further supplemented with 25 μl of a 100X dimethyl sulfoxide (DMSO) solution of the compound; the solution is diluted 100-fold in the supernatant of the cell culture, thus resulting in the anticipated SGK1-inhibitor concentration at a 1% DMSO concentration.
Animal Study:^{^[2]}	Animal Models 8-week-old wild type mice Dosages 20 mg/kg, 600 mg/kg Administration IP, Oral gavage

Cell Assay:^{^[1]}

Cell lines
HeLa-cells
Concentrations
0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time
24 h
Method
The cells are plated in 6-wells MTPs at a density of 10–20 × 10³ cells/cm² in Dulbecco´s DMEM medium, supplemented with 10% fetal calf serum (FCS), 2 mM glutamine and 1 mM sodium pyruvate. After 24 hrs at 37℃ and 5% CO₂ in a cell incubator, each well is further supplemented with 25 μl of a 100X dimethyl sulfoxide (DMSO) solution of the compound; the solution is diluted 100-fold in the supernatant of the cell culture, thus resulting in the anticipated SGK1-inhibitor concentration at a 1% DMSO concentration.

Animal Study:^{^[2]}

Animal Models
8-week-old wild type mice
Dosages
20 mg/kg, 600 mg/kg
Administration
IP, Oral gavage

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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