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

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.650mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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. This compound exhibits antihypertensive potency and anti-tumour activity.

Targets

SGK1
(Cell-free assay)

3 μM

In vitro

In vitro testing discloses EMD638683 as a SGK1 inhibitor with an IC50 of 3 μM. This compound 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.

In Vivo

The in vivo development of tumours following chemical carcinogenesis is significantly blunted by treatment with EMD638683. Within 24 hours in vivo this compound treatment significantly decreases blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.

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 this 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 this 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

https://pubmed.ncbi.nlm.nih.gov/21865856/
https://pubmed.ncbi.nlm.nih.gov/24081014/

Sellecks EMD638683 Has Been Cited by 1 Publication

Nedd4L signaling contributes to carbon tetrachloride-induced liver fibrosis in female mice and is associated with enteric dysbacteriosis [ Gastroenterol Rep (Oxf), 2025, 13:goaf022]	PubMed: 40066318

Nedd4L signaling contributes to carbon tetrachloride-induced liver fibrosis in female mice and is associated with enteric dysbacteriosis [ Gastroenterol Rep (Oxf), 2025, 13:goaf022]

PubMed: 40066318

RETURN POLICY
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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.