PI3K

Another significantly large group of kinases that regulate the transfer phosphate groups to hydroxyl groups of substrates is the class of PI3K’s (Phosphatidylinositide 3-kinases, EC 2.7.1.153), a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking. The family may be divided into three different classes (I-III), based on primary structure, regulation, and in vitro lipid substrate specificity[1]. PI3K’s play a crucial role in the PI3K/AKT/mTOR signaling pathway which is strongly involved in the fundamental cellular processes of protein synthesis and apoptosis. Disturbed activation of this intracellular pathway has been associated with the development of diseases such as cancer, diabetes mellitus, and autoimmunity[2]. Upon activation of phosphatidylinositol (PI)-3-kinase by extracellular growth factors, phosphorylation of the inner membrane phosphoinositides activates AKT (also known as Protein Kinase B, PKB) and PDPK1 (3-phosphoinositide dependent protein kinase-1).


[1] PI3K/Akt/mTOR pathway as a target for cancer therapy. D. Morgensztern, H.L. McLeod Drugs 2005, 16, 797–803
[2] PI3K-Akt pathway: its functions and alterations in human cancer. Osaki M, Oshimura M, Ito H. Apoptosis 2004, 9, 667-676.

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Axon ID Name Description From price
2994 GNE 317 Brain-penetrant PI3K inhibitor (p110-α specific) €85.00
1596 GSK 2126458 Dual PI3K and mTOR inhibitor €50.00
1912 GSK 2636771 dihydrochloride PI3K inhibitor (p110 β specific) €105.00
2168 IC 87114 Potent and highly selective inhibitor of the PI3K p110δ €85.00
2869 LX2343 BACE 1 inhibitor €125.00
1366 LY 294002 PI3K inhibitor €70.00
3098 ME-401 Potent, selective and orally available PI3K inhibitor (p110 δ specific) €100.00
3268 Metapristone Metabolite of Mifepristone (Axon 1502); PI3K/AKT inhibitor  Recently added €110.00
3247 Miltefosine PI3K/Akt inhibitor €50.00
1520 NVP-BBD130 Dual PI3K and mTOR kinase inhibitor €125.00
2029 NVP-BGT226 Orally active dual PI3K/mTOR inhibitor €120.00
1797 NVP-BKM120 Class I PI3K inhibitor €90.00
2610 PDK1 inhibitor 2610 Dual PI3K/PDPK1 inhibitor; desmethyl analogue of Axon 1282 €125.00
1855 PF 04691502 PI3K and mTOR tyrosine kinase inhibitor €90.00
1380 PI 103 hydrochloride PI3K inhibitor (p110 specific) €60.00

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