Kinases (Serine-Threonine Specific Protein)

The reversible phosphorylation of proteins represents a major post-translational signaling mechanism and regulatory pathway that controls a diverse set of cellular processes. The mode of action of these protein kinases is the reversible hydroxyl-phosphorylation of tyrosine, serine, and/or threonine residues of protein substrates. Since most kinases are specifically targeting tyrosine substrates, or serine/threonine substrates, the Axon Ligands™ in this catalogue targeting kinases have been subdivided into the two corresponding classes.Moreover, often the protein kinase itself is the substrate for an upstream kinase or undergoes auto-phosphorylation as part of a cascade of protein kinase signaling within the cell. Some representative protein kinase signaling pathways within cells include growth factor signaling and stress-activated signaling responses. Such pathways are highly interconnected and complex and regulate numerous cellular functions such as gene transcription, cell growth, proliferation, and differentiation. Signaling pathways of interest that will be highlighted individually are the DNA-damage response, the PI3K/AKT/mTOR pathway, the MAPK/ERK pathway, the NF-κB pathway, the TGF-β pathway, and the Wnt/β-Catenin pathway. Aberrant protein kinase activity can disrupt the normal control of cellular phosphorylation signaling pathways and lead to tumor formation. Given the critical role that protein kinases have in modulating cellular functions such as tumorigenesis, this class of enzymes has been targeted for the discovery and design of biologics and small-molecule inhibitors as potential therapeutic agents[1].


[1] Therapeutic Protein Kinase Inhibitors. S. K. Grant. Cell. Mol. Life Sci. 2009, 66, 1163 – 1177. 

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Axon ID Name Description From price
2540 Akt Inhibitor VIII Inhibitor of Akt1 and 2 with significant off-side effects (CaMKIα and AhR) €125.00
1859 AZD 5363 dihydrochloride Inhibitor of protein kinase B (Akt) €110.00
1561 AZD 8055 mTOR inhibitor €95.00
1282 BAG 956 PI3K and PDPK1 inhibitor €95.00
1281 BEZ 235 PI3K and mTOR tyrosine kinase inhibitor €60.00
1390 BX 795 PDPK1, TBK1 and IKK inhibitor €60.00
1130 BX 912 PDPK1 inhibitor €60.00
1239 Deguelin Akt inhibitor €95.00
2630 eCF309 Highly selective and potent inhibitor of mTOR signalling €85.00
1782 GDC 0980 Dual PI3K and mTOR inhibitor €105.00
2460 GSK 2110183 hydrochloride Potent, reversible, selective, and orally bioavailable inhibitor of the Akt kinases €105.00
1596 GSK 2126458 Dual PI3K and mTOR inhibitor €80.00
1729 GSK 690693 ATP-competitive pan-Akt kinase inhibitor €115.00
3007 GSK 8612 Potent and highly selective TBK1 inhibitor €120.00
2142 INK 128 Potent and selective mTOR inhibitor €110.00

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