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Submit ReviewGSK 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.
Sold for research purposes only under agreement from GlaxoSmithKline
GSK 690693 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 425.48 |
公式 | C21H27N7O3 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 21.27 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: GSK 690693, GSK 690693 supplier, GSK, 690693, inhibits, Akt, inhibitors, GSK690693, antitumor, antiproliferative, (Protein, Kinase, B), Protein, B/Akt, 4144, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GSK 690693 的部分引用包括:
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
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GSK 690693 inhibitor was used in studies exploring the role of drug-induced activation of Akt kinase in pancreatic cancer cells. Results were consistent.