The pleiotropic actions of insulin are mediated by a single receptor tyrosine kinase (RTK class II, Insulin receptor family). A generally accepted paradigm is that insulin receptors, acting through insulin receptor substrates (insulin, and Insulin-like growth factors (IGF) I and II), stimulate the lipid kinase activity of phosphatidylinositol 3-kinase (PI3K)[1]. The rapid rise in Tris-phosphorylated inositol (PIP3) that ensues triggers a cascade of PIP3-dependent serine/threonine kinases. Among the latter, Akt  and atypical protein kinase C isoforms are thought to be involved in insulin regulation of glucose transport and oxidation; glycogen, lipid, and protein synthesis; and modulation of gene expression. "Insulin insensitivity", or a decrease in insulin receptor signaling, leads to diabetes mellitus type 2 – the cells are unable to take up glucose, and the result is hyperglycemia (an increase in circulating glucose), and all the sequelae that result from diabetes.

[1] The Insulin Receptor and Its Cellular Targets. Y. Kido, J. Nakae, D. Accili. J. Clin.Endocrin. Met. 2001, 86, 972-979.

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2267 GSK 1838705A Potent IGF-IR and insulin receptor (IR) kinase inhibitor with additional affinity for ALK €110.00
3830 GSK1904529A Potent, selective and orally active inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) Inquire
2238 NT 157 Unique allosteric inhibitor of IGF1R signaling €95.00
1702 OSI 906 IGF1R tyrosine kinase inhibitor €60.00
3341 PQ401 Potent IGF1R tyrosine kinase inhibitor €100.00
3866 TAE226 Potent and ATP-competitive dual FAK and IGF-1R inhibitor €110.00
3973 XL-228 Multitargeted protein kinase inhibitor (IGF1R, Aurora,FGFR, ABL,ALK and SRC) Inquire

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