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[CAS NO. 1181770-72-8] EMD638683
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15193 |
| Brand: | MCE |
| CAS: | 1181770-72-8 |
Overview
| MDL | MFCD25541743 |
|---|---|
| Molecular Weight | 364.34 |
| Molecular Formula | C18H18F2N2O4 |
| SMILES | CC1=C(CC)C(C(NNC(C(O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O |
12 Publications Citing Use of MCE
- [1]J Infection. 2022 Nov 2;S0163-4453(22)00635-1.
- [2]Adv Sci (Weinh). 2021 Nov 10;e2101485.
- [3]Signal Transduct Target Ther. 2022 Jul 27;7(1):255.
- [4]J Autoimmun. 2016 Feb;67:90-101.
- [5]J Bone Miner Res. 2015 Nov;30(11):1959-68.
- [6]Cancer Biol Med. 2021 May 7;j.issn.2095-3941.2020.0430.
- [7]FASEB J. 2015 Sep;29(9):3737-49.
- [8]J Immunol. 2021 Jun 23;ji2001455.
- [9]Mol Neurobiol. 2021 Mar;58(3):964-982.
- [10]J Biol Chem. 2022 May 16;102036.
- [11]Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8.
- [12]Acta Biochim Biophys Sin (Shanghai). 2017 Apr 1;49(4):302-310.
Summary
EMD638683 is a highly selective SGK1 inhibitor, with an IC 50 value of 3 μM.
IC50 & Target
|
SGK1
|
In Vitro
EMD638683 is a SGK1 inhibitor. EMD638683 inhibits the NDRG1 (N-Myc downstream-regulated gene 1) phosphorylation, an effect requiring 3.35±0.32 μM EMD638683 in the cell culture medium for half maximal effect (IC 50 ). EMD638683 has also an inhibitory effect on cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), and the SGK isoforms SGK2 and SGK3 [1] . In both, control and EMD638683 (50 µM)-treated CaCo-2 cells, radiation significantly increases the percentage of CaCo-2 cells undergoing late apoptosis. EMD638683 treatment alone tends to enhance the percentage of apoptotic CaCo-2 cells. Following radiation the percentage of apoptotic EMD638683-treated CaCo-2 cells is significantly higher than the percentage of apoptotic control cells. Thus, EMD638683 treatment significantly augments the apoptosis following radiation [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 137.23 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
References
- [1] Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46.
- [2] Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48.
- [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.
- [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.
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