Cat. No.: HY-15193

EMD638683

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

EMD638683 is an orally active SGK1 inhibitor with an IC₅₀ of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer.

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Pureté: 99.94%
CAS No.: 1181770-72-8
Formule: C₁₈H₁₈F₂N₂O₄
Masse moléculaire:364.34

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

EMD638683 Chemical Structure

CAS No.: 1181770-72-8

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[3]

SGK1

3 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform SGK :

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR) :

Voir tous les produits spécifiques à Isoform Interleukin Related :

In Vitro

EMD638683 (50 μM; 9-25 h) inhibits NLRP3 inflammasome activation and IL-1β secretion in mouse bone marrow-derived macrophages induced by angiotensin II (Ang II) by targeting NLRP3 expression^[2].
EMD638683 (50 μM; 25-49 h) inhibits angiotensin II-induced transformation of primary mouse cardiac fibroblasts into myofibroblasts by reducing IL-1β secretion from macrophages^[2].
EMD638683 (50 μM; 96 h) enhances radiation-induced apoptotic death of Caco-2 colon cancer cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[3]

Cell Line:

Caco-2 cells
Concentration:

50 μM
Incubation Time:

24 h pre-incubation, 72 h post-radiation incubation
Result:

Enhanced radiation-induced apoptotic cell death in Caco-2 colon carcinoma cells, including augmented cell shrinkage, mitochondrial depolarization, caspase 3 activation, phosphatidylserine exposure, and late apoptosis.

In Vivo

EMD638683 (600 mg/kg, administered via mixed diet for 4 consecutive days) normalizes systolic blood pressure in hyperinsulinemic, salt-loaded wild-type mice, reducing their blood pressure from 111 mmHg to 87 mmHg over the 4-day treatment period^[1].
EMD638683 (600 mg/kg, administered via mixed feed for 4 weeks) prevents hypertension in wild-type mice treated with 10% fructose in isotonic saline for 4 weeks^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 4 months old, hyperinsulinemic salt-loaded)^[1]
Dosage:

600 mg/kg
Administration:

p.o.; continuous in chow; 4 days
Result:

Normalized systolic blood pressure from 111 mmHg to 87 mmHg.
Significantly increased urinary flow rate.
Significantly decreased body weight.
Caused no significant changes to fluid intake, food intake, or urinary Na+ and K+ excretion.
Increased blood pressure to 106 mmHg after returning to placebo food.

Animal Model:

SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 7 to 10 months old, fructose/salt-induced hypertension)^[1]
Dosage:

600 mg/kg
Administration:

p.o.; continuous in chow; 4 weeks
Result:

Prevented the fructose/salt-induced rise in systolic blood pressure.
Resulted in significantly lower systolic blood pressure compared to placebo-treated mice.

Chemical Information

CAS No. 1181770-72-8
Appearance Solid
Masse moléculaire 364.34
Formule C₁₈H₁₈F₂N₂O₄
Color Off-white to light brown
SMILES

CC1=C(CC)C(C(NNC(C(O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All WB

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Journal Impact Factor

Signal Transduct Target Ther

SARS-CoV-2 envelope protein impairs airway epithelial barrier function and exacerbates airway inflammation via increased intracellular Cl- concentration. [Abstract]

2024 Mar 25;9(1):74. PMID: 38528022
Signal Transduct Target Ther

SARS-CoV-2 nucleocapsid protein triggers hyperinflammation via protein-protein interaction-mediated intracellular Cl- accumulation in respiratory epithelium. [Abstract]

2022 Jul 27;7(1):255. PMID: 35896532
Adv Sci (Weinh)

Discovery of Herbacetin as a Novel SGK1 Inhibitor to Alleviate Myocardial Hypertrophy. [Abstract]

2022 Jan;9(2):e2101485. PMID: 34761560
Cancer Biol Med

Complement C3a activates osteoclasts by regulating the PI3K/PDK1/SGK3 pathway in patients with multiple myeloma. [Abstract]

2021 May 7;18(3):721-733. PMID: 33960177
Int J Biol Sci

SGK1 aggravates idiopathic pulmonary fibrosis by triggering H3k27ac-mediated macrophage reprogramming and disturbing immune homeostasis. [Abstract]

2024 Jan 12;20(3):968-986. PMID: 38250161
Phytomedicine

Berbamine alleviates neuropathic pain via suppressing spinal TMEM34/SGK1/FOXO3 axis. [Abstract]

2025 May:140:156619. PMID: 40088745
J Infection

Toxoplasma gondii infection triggers ongoing inflammation mediated by increased intracellular Cl- concentration in airway epithelium. [Abstract]

2022 Nov 2;S0163-4453(22)00635-1. PMID: 36334726
J Med Chem

Brain Permeable SGK1 Inhibitors: A Promising Therapeutic Strategy for Neurodegenerative Diseases. [Abstract]

2026 Mar 16. PMID: 41837733
J Autoimmun

Sodium chloride promotes pro-inflammatory macrophage polarization thereby aggravating CNS autoimmunity. [Abstract]

2016 Feb:67:90-101. PMID: 26584738
J Bone Miner Res

PTH Promotes Bone Anabolism by Stimulating Aerobic Glycolysis via IGF Signaling. [Abstract]

2015 Nov;30(11):1959-68. PMID: 25990470
Mol Neurobiol

NGF-Induced Nav1.7 Upregulation Contributes to Chronic Post-surgical Pain by Activating SGK1-Dependent Nedd4-2 Phosphorylation. [Abstract]

2021 Mar;58(3):964-982. PMID: 33063281
Environ Toxicol Pharmacol

Increased expression and activation of serum- and glucocorticoid-inducible kinase-1 (SGK1) by cadmium in HK-2 renal proximal tubular epithelial cells. [Abstract]

2014 Sep;38(2):374-8. PMID: 25128767

EMD638683 purchased from MedChemExpress. Usage Cited in: Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8. [Abstract]

Effects of EMD638683 and SGK1 knockdown on the CdCl2-induced phosphorylation of SGK1, NDRG1, FoxO3a, andCREB in HK-2 cells. Cells are incubated with 50 μM EMD638683 for 1 h and then incubated with or without 20 μM CdCl₂ for 8 h.
Acta Biochim Biophys Sin (Shanghai)

Response of human non-small-cell lung cancer cells to the influence of Wogonin with SGK1 dynamics. [Abstract]

2017 Apr 1;49(4):302-310. PMID: 28338770

EMD638683 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2017 Apr 1;49(4):302-310. [Abstract]

The expression levels of SGK1 at different concentrations of Wogonin and EMD638683 are assayed using western blot with GAPDH as an internal control.
FASEB J

Inhibition of serum- and glucocorticoid-inducible kinase 1 enhances TLR-mediated inflammation and promotes endotoxin-driven organ failure. [Abstract]

2015 Sep;29(9):3737-49. PMID: 25993992

EMD638683 purchased from MedChemExpress. Usage Cited in: FASEB J. 2015 Sep;29(9):3737-49. [Abstract]

Phosphorylation of NDRG-1 is completely suppressed by 10 μM EMD638683 in human monocytes upon LPS stimulation. Whole cell lysates of purified human monocytes upon LPS stimulation and EMD638683 pre-treatment are probed for phosphorylation of the SGK1 substrate, NDRG, and total GAPDH by Western Blot.
J Biol Chem

SGK1 negatively regulates inflammatory immune responses and protects against alveolar bone loss through modulation of TRAF3 activity. [Abstract]

2022 Jun;298(6):102036. PMID: 35588785
J Immunol

Serum- and Glucocorticoid-Inducible Kinase 1 Promotes Alternative Macrophage Polarization and Restrains Inflammation through FoxO1 and STAT3 Signaling. [Abstract]

2021 Jul 1;207(1):268-280. PMID: 34162726
Immun Inflamm Dis

Identification and Functional Analysis of PANoptosis-Associated Genes in the Progression From Sepsis to ARDS. [Abstract]

2025 Jan;13(1):e70136. PMID: 39854144
J Vasc Dis

2026 Feb;5(1):10.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (137.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7447 mL

13.7234 mL

27.4469 mL

5 mM

0.5489 mL

2.7447 mL

5.4894 mL

10 mM

0.2745 mL

1.3723 mL

2.7447 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46. [Content Brief]

[2]. Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48. [Content Brief]

[3]. Gan W, et al. The SGK1 inhibitor EMD638683, prevents Angiotensin II-induced cardiac inflammation and fibrosis by blocking NLRP3 inflammasome activation. Biochim Biophys Acta Mol Basis Dis. 2018;1864(1):1-10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7447 mL	13.7234 mL	27.4469 mL	68.6172 mL
	5 mM	0.5489 mL	2.7447 mL	5.4894 mL	13.7234 mL
	10 mM	0.2745 mL	1.3723 mL	2.7447 mL	6.8617 mL
	15 mM	0.1830 mL	0.9149 mL	1.8298 mL	4.5745 mL
	20 mM	0.1372 mL	0.6862 mL	1.3723 mL	3.4309 mL
	25 mM	0.1098 mL	0.5489 mL	1.0979 mL	2.7447 mL
	30 mM	0.0915 mL	0.4574 mL	0.9149 mL	2.2872 mL
	40 mM	0.0686 mL	0.3431 mL	0.6862 mL	1.7154 mL
	50 mM	0.0549 mL	0.2745 mL	0.5489 mL	1.3723 mL
	60 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1436 mL
	80 mM	0.0343 mL	0.1715 mL	0.3431 mL	0.8577 mL
	100 mM	0.0274 mL	0.1372 mL	0.2745 mL	0.6862 mL

Keywords

EMD638683

18 Cited Publications

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EMD638683

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Human Metabolite Library

Pain-Related Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Inflammasomes related Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) EMD638683

Voir tous les produits spécifiques à Isoform SGK

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR)

Voir tous les produits spécifiques à Isoform Interleukin Related

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

EMD638683 Related Classifications

HY-15193 Related Classifications