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.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1831 | A 66 | PI3K inhibitor (p110-α specific) | €95.00 | |
2857 | Acalisib | PI3K inhibitor (p110 δ specific) | €120.00 | |
2925 | Alpelisib | PI3K inhibitor (p110-α specific) | €90.00 | |
3827 | AMG-511 | Orally bioavailable, highly potent and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor | Inquire | |
1424 | AS 252424 | PI3K inhibitor (p110-γ specific) | €85.00 | |
1436 | AS 252424 bispotassium salt | PI3K inhibitor (p110-γ specific) | €95.00 | |
2748 | Autophinib | PIK3C3/Vps34 inhibitor | €120.00 | |
3808 | AZD3458 | Orally bioavailable potent and selective PI3Kγ inhibitor | Inquire | |
2926 | AZD6482 | PI3K inhibitor (p110 β specific) | €120.00 | |
3690 | AZD8186 | PI3Kβ/δ isoform-selective inhibitor | Inquire | |
3055 | B591 | Potent, specific class I PI3K inhibitor | €125.00 | |
1282 | BAG 956 | PI3K and PDPK1 inhibitor | €95.00 | |
3942 | BAY-1082439 | PI3Kα/β-balanced inhibitor | Inquire | |
1281 | BEZ 235 | PI3K and mTOR tyrosine kinase inhibitor | €50.00 | |
2170 | CAL 101 | PI3K inhibitor (p110 δ specific) | €95.00 | |
2039 | CZC 24832 | PI3K inhibitor (p110-γ specific) | €95.00 | |
1719 | D 106669 | Potent and selective PI3K inhibitor | €85.00 | |
1377 | GDC 0941 bismesylate | PI3K inhibitor | €80.00 | |
1782 | GDC 0980 | Dual PI3K and mTOR inhibitor | €80.00 | |
2994 | GNE 317 | Brain-penetrant PI3K inhibitor (p110-α specific) | €85.00 | |
3807 | GS-9901 | Potent and isoform-selective inhibitor of PI3Kδ | Inquire | |
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 | |
4133 | IPI-145 | PI3K p110α/γ isoform specific inhibitor | Inquire | |
4147 | IPI-549 | Orally bioavailable potent and selective PI3Kγ inhibitor | Inquire | |
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 | €110.00 |