EMD638683
EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 μM. 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. EMD638683 promotes radiation-induced suicidal death of colon tumor cells in vitro and decreases the number of colonic tumors following chemical carcinogenesis in vivo.
1: Inoue K, Leng T, Yang T, Zeng Z, Ueki T, Xiong ZG. Role of serum- and glucocorticoid-inducible kinases in stroke. J Neurochem. 2016 Jul;138(2):354-61. doi: 10.1111/jnc.13650. Epub 2016 May 25. PubMed PMID: 27123541; PubMed Central PMCID: PMC4936920.
2: Zhang B, Umbach AT, Chen H, Yan J, Fakhri H, Fajol A, Salker MS, Spichtig D, Daryadel A, Wagner CA, Föller M, Lang F. Up-regulation of FGF23 release by aldosterone. Biochem Biophys Res Commun. 2016 Feb 5;470(2):384-90. doi: 10.1016/j.bbrc.2016.01.034. Epub 2016 Jan 8. PubMed PMID: 26773502.
3: Voelkl J, Castor T, Musculus K, Viereck R, Mia S, Feger M, Alesutan I, Lang F. SGK1-Sensitive Regulation of Cyclin-Dependent Kinase Inhibitor 1B (p27) in Cardiomyocyte Hypertrophy. Cell Physiol Biochem. 2015;37(2):603-14. PubMed PMID: 26344141.
4: Yan J, Schmid E, Almilaji A, Shumilina E, Borst O, Laufer S, Gawaz M, Lang F. Effect of TGFβ on calcium signaling in megakaryocytes. Biochem Biophys Res Commun. 2015 May 22;461(1):8-13. doi: 10.1016/j.bbrc.2015.03.159. Epub 2015 Apr 4. PubMed PMID: 25849886.
5: Liu G, Honisch S, Liu G, Schmidt S, Pantelakos S, Alkahtani S, Toulany M, Lang F, Stournaras C. Inhibition of SGK1 enhances mAR-induced apoptosis in MCF-7 breast cancer cells. Cancer Biol Ther. 2015;16(1):52-9. doi: 10.4161/15384047.2014.986982. PubMed PMID: 25427201; PubMed Central PMCID: PMC4622018.
6: Hosseinzadeh Z, Schmid E, Shumilina E, Laufer S, Borst O, Gawaz M, Lang F. Effect of TGFβ on Na+/K+ ATPase activity in megakaryocytes. Biochem Biophys Res Commun. 2014 Sep 26;452(3):537-41. doi: 10.1016/j.bbrc.2014.08.093. Epub 2014 Aug 27. PubMed PMID: 25168590.
7: Miyayama T, Matsuoka M. Increased expression and activation of serum- and glucocorticoid-inducible kinase-1 (SGK1) by cadmium in HK-2 renal proximal tubular epithelial cells. Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8. doi: 10.1016/j.etap.2014.07.004. Epub 2014 Jul 16. PubMed PMID: 25128767.
8: Schmidt S, Liu G, Liu G, Yang W, Honisch S, Pantelakos S, Stournaras C, Hönig A, Lang F. Enhanced Orai1 and STIM1 expression as well as store operated Ca2+ entry in therapy resistant ovary carcinoma cells. Oncotarget. 2014 Jul 15;5(13):4799-810. PubMed PMID: 25015419; PubMed Central PMCID: PMC4148100.
9: Xi X, Liu S, Shi H, Yang M, Qi Y, Wang J, Du J. 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. doi: 10.1007/s12012-014-9260-4. PubMed PMID: 24825325.
10: Chatterjee S, Schmidt S, Pouli S, Honisch S, Alkahtani S, Stournaras C, Lang F. Membrane androgen receptor sensitive Na+/H+ exchanger activity in prostate cancer cells. FEBS Lett. 2014 May 2;588(9):1571-9. doi: 10.1016/j.febslet.2014.02.040. Epub 2014 Mar 4. PubMed PMID: 24607544.
11: Munoz C, Pakladok T, Almilaji A, Elvira B, Decher N, Shumilina E, Lang F. Up-regulation of Kir2.1 (KCNJ2) by the serum & glucocorticoid inducible SGK3. Cell Physiol Biochem. 2014;33(2):491-500. doi: 10.1159/000358629. Epub 2014 Feb 14. PubMed PMID: 24556932.
12: Liu G, Liu G, Alzoubi K, Umbach AT, Pelzl L, Borst O, Gawaz M, Lang F. Upregulation of store operated Ca channel Orai1, stimulation of Ca(2+) entry and triggering of cell membrane scrambling in platelets by mineralocorticoid DOCA. Kidney Blood Press Res. 2013;38(1):21-30. doi: 10.1159/000355750. Epub 2014 Feb 2. PubMed PMID: 24525794.
13: Towhid ST, Liu GL, Ackermann TF, Beier N, Scholz W, Fuchß T, Toulany M, Rodemann HP, Lang F. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48. doi: 10.1159/000354486. Epub 2013 Sep 20. PubMed PMID: 24081014.
14: Voelkl J, Pasham V, Ahmed MS, Walker B, Szteyn K, Kuhl D, Metzler B, Alesutan I, Lang F. Sgk1-dependent stimulation of cardiac Na+/H+ exchanger Nhe1 by dexamethasone. Cell Physiol Biochem. 2013;32(1):25-38. doi: 10.1159/000350120. Epub 2013 Jul 4. PubMed PMID: 23860121.
15: Ackermann TF, Boini KM, Beier N, Scholz W, Fuchss T, Lang F. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46. doi: 10.1159/000331722. Epub 2011 Aug 16. PubMed PMID: 21865856.
2: Zhang B, Umbach AT, Chen H, Yan J, Fakhri H, Fajol A, Salker MS, Spichtig D, Daryadel A, Wagner CA, Föller M, Lang F. Up-regulation of FGF23 release by aldosterone. Biochem Biophys Res Commun. 2016 Feb 5;470(2):384-90. doi: 10.1016/j.bbrc.2016.01.034. Epub 2016 Jan 8. PubMed PMID: 26773502.
3: Voelkl J, Castor T, Musculus K, Viereck R, Mia S, Feger M, Alesutan I, Lang F. SGK1-Sensitive Regulation of Cyclin-Dependent Kinase Inhibitor 1B (p27) in Cardiomyocyte Hypertrophy. Cell Physiol Biochem. 2015;37(2):603-14. PubMed PMID: 26344141.
4: Yan J, Schmid E, Almilaji A, Shumilina E, Borst O, Laufer S, Gawaz M, Lang F. Effect of TGFβ on calcium signaling in megakaryocytes. Biochem Biophys Res Commun. 2015 May 22;461(1):8-13. doi: 10.1016/j.bbrc.2015.03.159. Epub 2015 Apr 4. PubMed PMID: 25849886.
5: Liu G, Honisch S, Liu G, Schmidt S, Pantelakos S, Alkahtani S, Toulany M, Lang F, Stournaras C. Inhibition of SGK1 enhances mAR-induced apoptosis in MCF-7 breast cancer cells. Cancer Biol Ther. 2015;16(1):52-9. doi: 10.4161/15384047.2014.986982. PubMed PMID: 25427201; PubMed Central PMCID: PMC4622018.
6: Hosseinzadeh Z, Schmid E, Shumilina E, Laufer S, Borst O, Gawaz M, Lang F. Effect of TGFβ on Na+/K+ ATPase activity in megakaryocytes. Biochem Biophys Res Commun. 2014 Sep 26;452(3):537-41. doi: 10.1016/j.bbrc.2014.08.093. Epub 2014 Aug 27. PubMed PMID: 25168590.
7: Miyayama T, Matsuoka M. Increased expression and activation of serum- and glucocorticoid-inducible kinase-1 (SGK1) by cadmium in HK-2 renal proximal tubular epithelial cells. Environ Toxicol Pharmacol. 2014 Sep;38(2):374-8. doi: 10.1016/j.etap.2014.07.004. Epub 2014 Jul 16. PubMed PMID: 25128767.
8: Schmidt S, Liu G, Liu G, Yang W, Honisch S, Pantelakos S, Stournaras C, Hönig A, Lang F. Enhanced Orai1 and STIM1 expression as well as store operated Ca2+ entry in therapy resistant ovary carcinoma cells. Oncotarget. 2014 Jul 15;5(13):4799-810. PubMed PMID: 25015419; PubMed Central PMCID: PMC4148100.
9: Xi X, Liu S, Shi H, Yang M, Qi Y, Wang J, Du J. 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. doi: 10.1007/s12012-014-9260-4. PubMed PMID: 24825325.
10: Chatterjee S, Schmidt S, Pouli S, Honisch S, Alkahtani S, Stournaras C, Lang F. Membrane androgen receptor sensitive Na+/H+ exchanger activity in prostate cancer cells. FEBS Lett. 2014 May 2;588(9):1571-9. doi: 10.1016/j.febslet.2014.02.040. Epub 2014 Mar 4. PubMed PMID: 24607544.
11: Munoz C, Pakladok T, Almilaji A, Elvira B, Decher N, Shumilina E, Lang F. Up-regulation of Kir2.1 (KCNJ2) by the serum & glucocorticoid inducible SGK3. Cell Physiol Biochem. 2014;33(2):491-500. doi: 10.1159/000358629. Epub 2014 Feb 14. PubMed PMID: 24556932.
12: Liu G, Liu G, Alzoubi K, Umbach AT, Pelzl L, Borst O, Gawaz M, Lang F. Upregulation of store operated Ca channel Orai1, stimulation of Ca(2+) entry and triggering of cell membrane scrambling in platelets by mineralocorticoid DOCA. Kidney Blood Press Res. 2013;38(1):21-30. doi: 10.1159/000355750. Epub 2014 Feb 2. PubMed PMID: 24525794.
13: Towhid ST, Liu GL, Ackermann TF, Beier N, Scholz W, Fuchß T, Toulany M, Rodemann HP, Lang F. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48. doi: 10.1159/000354486. Epub 2013 Sep 20. PubMed PMID: 24081014.
14: Voelkl J, Pasham V, Ahmed MS, Walker B, Szteyn K, Kuhl D, Metzler B, Alesutan I, Lang F. Sgk1-dependent stimulation of cardiac Na+/H+ exchanger Nhe1 by dexamethasone. Cell Physiol Biochem. 2013;32(1):25-38. doi: 10.1159/000350120. Epub 2013 Jul 4. PubMed PMID: 23860121.
15: Ackermann TF, Boini KM, Beier N, Scholz W, Fuchss T, Lang F. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46. doi: 10.1159/000331722. Epub 2011 Aug 16. PubMed PMID: 21865856.
| Chemical | |
|---|---|
| CAS Num | 1181770-72-8 |
| Chemical Formula | C18H18F2N2O4 |
| Molecular Weight | 364.3488 |
| IUPAC Chemical Name | N'-[2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide |
| Exact Mass | 364.1235 |
| Elemental Analysis | C, 59.34; H, 4.98; F, 10.43; N, 7.69; O, 17.56 |
| Synonym | EMD638683; EMD 638683; EMD-638683. |
| Solubility | Soluble in DMSO |
| SMILES Code | O=C(NNC(C(C1=CC(F)=CC(F)=C1)O)=O)C2=CC=C(O)C(C)=C2CC |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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