GSK 690693

Pricing Availability   Qty
Description: Akt kinase inhibitor. Antitumor
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% (HPLC)
Datasheet
Citations (5)
Reviews (1)
Pathways (1)

Biological Activity for GSK 690693

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.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Compound Libraries for GSK 690693

GSK 690693 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 690693

M. Wt 425.48
Formula C21H27N7O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 937174-76-0
PubChem ID 90488916
InChI Key WONPMIMNXYCXKK-AWEZNQCLSA-N
Smiles NC1=NON=C1C(N3CC)=NC2=C3C(CO[C@@H]4CNCCC4)=CN=C2C#CC(C)(C)O

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.

Solubility Data for GSK 690693

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.27 50

Preparing Stock Solutions for GSK 690693

The following data is based on the product molecular weight 425.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.7 mL 23.5 mL 47.01 mL
2.5 mM 0.94 mL 4.7 mL 9.4 mL
5 mM 0.47 mL 2.35 mL 4.7 mL
25 mM 0.09 mL 0.47 mL 0.94 mL

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Product Datasheets for GSK 690693

Certificate of Analysis / Product Datasheet
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References for GSK 690693

References are publications that support the biological activity of the product.

Heerding et al (2008) 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. J.Med.Chem. 51 5663 PMID: 18800763

Rhodes et al (2008) Characterization of an Akt inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res. 68 2366 PMID: 18381444


If you know of a relevant reference for GSK 690693, please let us know.

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View all Akt (Protein Kinase B) Inhibitors

Keywords: GSK 690693, GSK 690693 supplier, GSK, 690693, inhibits, Akt, inhibitors, GSK690693, antitumor, antiproliferative, (Protein, Kinase, B), Protein, B/Akt, 4144, Tocris Bioscience

5 Citations for GSK 690693

Citations are publications that use Tocris products. Selected citations for GSK 690693 include:

Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. J Mol Neurosci 10 e0143319 PMID: 26619345

Nissa et al (2018) Reduction of protein kinase A-mediated phosphorylation of ATXN1-S776 in Purkinje cells delays onset of Ataxia in a SCA1 mouse model. Neurobiol Dis 116 93-105 PMID: 29758256

Marisa et al (2013) α1β1 integrin/Rac1-dependent mesangial invasion of glomerular capillaries in Alport syndrome. Am J Pathol 183 1269-1280 PMID: 23911822

Sokołowska et al (2014) Orexins protect neuronal cell cultures against hypoxic stress: an involvement of Akt signaling. Stem Cell Reports 52 48 PMID: 24243084

Khuituan et al (2012) Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice. Am J Physiol Endocrinol Metab 302 E903 PMID: 22275752


Do you know of a great paper that uses GSK 690693 from Tocris? Please let us know.

Reviews for GSK 690693

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Effects on Akt kinase activation in cancer.
By MARINA KOUTSIOUMPA on 10/18/2022
Assay Type: In Vitro
Species: Human

GSK 690693 inhibitor was used in studies exploring the role of drug-induced activation of Akt kinase in pancreatic cancer cells. Results were consistent.


Pathways for GSK 690693

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.