GSK 690693
Chemical Name: 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol
Purity: ≥98%
Biological Activity
GSK 690693 is an ATP-competitive pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM of Akt1, 2 and 3 respectively). Also exhibits some inhibition for AMPK, PKA and PAK and PKC isoforms (IC50 < 100 nM). Displays antiproliferative and apoptotic effects in tumor cell lines.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Gastrointestinal cancer cells treatment with bevacizumab activates a VEGF autoregulatory mechanism involving telomerase catalytic subunit hTERT via PI3K-AKT, HIF-1? and VEGF receptors
N Mahfouz, R Tahtouh, N Alaaeddine, J El Hajj, R Sarkis, R Hachem, I Raad, G Hilal
PLoS ONE, 2017;12(6):e0179202. -
Influenza A virus neuraminidase protein enhances cell survival through interaction with carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6) protein.
Gaur P, Ranjan P, Sharma S, Patel JR, Bowzard JB, Rahman SK, Kumari R, Gangappa S, Katz JM, Cox NJ, Lal RB, Sambhara S, Lal SK
J. Biol. Chem., 2012;287(18):15109-17. -
Identification of 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{(3S)-3-piperidinylmethoxyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Heerding et al.
J.Med.Chem., 2008;51:5663 -
Characterization of an Akt inhibitor with potent pharmacodynamic and antitumor activity.
Rhodes et al.
Cancer Res., 2008;68:2366
Product Datasheets
Citations for GSK 690693
The citations listed below are publications that use Tocris products. Selected citations for GSK 690693 include:
5 Citations: Showing 1 - 5
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Reduction of protein kinase A-mediated phosphorylation of ATXN1-S776 in Purkinje cells delays onset of Ataxia in a SCA1 mouse model.
Authors: Nissa Et al.
Neurobiol Dis 2018;116:93-105
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Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
Authors: Rogers and Gahring
J Mol Neurosci 2015;10:e0143319
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Orexins protect neuronal cell cultures against hypoxic stress: an involvement of Akt signaling.
Authors: Sokołowska Et al.
Stem Cell Reports 2014;52:48
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α1β1 integrin/Rac1-dependent mesangial invasion of glomerular capillaries in Alport syndrome.
Authors: Marisa Et al.
Am J Pathol 2013;183:1269-1280
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Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice.
Authors: Khuituan Et al.
Am J Physiol Endocrinol Metab 2012;302:E903
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