EMD638683

SKU: orb1300597

Description

EMD638683 is a potent and selective serum- and glucocorticoid-regulated kinase (SGK) inhibitor with an IC50 of 3 µM. This small molecule is a valuable research tool for investigating SGK1's role in hypertension, renal function, and cellular ion transport in both in vitro and in vivo models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1181770-72-8
• MW: 364.34
• Purity: 98.00% (May vary between batches)
• Formula: C₁₈H₁₈F₂N₂O₄
• SMILES: CCc1c(C)c(O)ccc1C(=O)NNC(=O)C(O)c1cc(F)cc(F)c1
• Target: SGK
• Solubility: DMSO:50 mg/mL (137.23 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.49 mM)

Bioactivity

• Target IC50:
  SGK1:3 μM
• 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.
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• In Vitro:
  EMD638683 treatment significantly augmented 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. The in vivo development of tumors following chemical carcinogenesis was significantly blunted by treatment with EMD638683.
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• Cell Research:
  Colon carcinoma (Caco-2) cells were exposed to EMD638683 with or without exposure to radiation (3 Gray) and cell volume was estimated from forward scatter, phosphatidylserine exposure from annexin V binding, mitochondrial potential from JC-9 fluorescence, caspase 3 activity from CaspGlow Fluorescein staining, DNA degradation from propidium iodide staining as well as late apoptosis from annexin-V FITC and propidium iodide double staining. In vivo tumor growth was determined in wild type mice subjected to chemical carcinogenesis (intraperitoneal injection of 20 mg/kg 1,2-dimethylhydrazine followed by three cycles of 30 g/L synthetic dextran sulfate sodium in drinking water for 7 days).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, EMD638683, EMD-638683, EMD 638683, inhibit, SGK1, SGK, Serum and glucocorticoid-regulated kinase, Serum-glucocorticoid regulated kinase

Compound Identifiers

PubChem CID

44182398

Sheyda Bahiraii er al. Role of Inositol Hexakisphosphate Kinases in Vascular Smooth Muscle Cell Calcification International Journal of Molecular Sciences, (2026)

PubMed: