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.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
4192 | (S)-BI 2536 | Dual PLK1/BRD4 bromodomain inhibitor | €170.00 | |
2786 | (±)-PH 797804 | Inhibitor of p38α MAPK | €115.00 | |
1892 | 1-NM-PP1 | Potent tyrosine kinase inhibitor (TKI) of multiple targets (Src, Fyn, Abl, CDK, Trk) | €95.00 | |
1902 | 4μ8C | IRE1α inhibitor | €105.00 | |
1909 | A 1070722 | Selective inhibitor of GSK-3 | €95.00 | |
1466 | A 769662 | AMPK activator | €85.00 | |
2720 | A-92 | Inhibitor of GCN2 (EIF2AK4) | €140.00 | |
1291 | AEG 3482 | JNK inhibitor | €90.00 | |
2389 | AICAR | Potent AMPK activator and inducer of differentiation of NSCs | €45.00 | |
3408 | AKI603 | Inhibitor of Aurora A kinase | €145.00 | |
2540 | Akt Inhibitor VIII | Inhibitor of Akt1 and 2 with significant off-side effects (CaMKIα and AhR) | €95.00 | |
2971 | Amcasertib | First-in-class stemness kinase inhibitor | €145.00 | |
1783 | AMG 900 | Aurora inhibitor (non-specific) | €110.00 | |
4071 | AMG-925 | Potent, selective, and orally available FLT3/CDK4 dual inhibitor | Inquire | |
2717 | Apigenin | Selective inhibitor of Casein kinase 2 (CK2) | €70.00 | |
3328 | APIO-EE-07 | Dual RSK1/MSK2 inhibitor | €140.00 | |
2611 | APS-2-79 | Inhibitor of KSR and oncogenic Ras signaling | €90.00 | |
2167 | AR-A 014418 | ATP-competitive GSK-3 inhibitor | €85.00 | |
3041 | ARN 3236 | Potent, selective, ATP-competitive, and orally available inhibitor of SIK2 | €80.00 | |
4264 | ART-446 | Potent CHK2 inhibitor | Inquire | |
2187 | AS 1892802 | Potent, selective, ATP-competitive ROCK inhibitor | €95.00 | |
2179 | ASK1 Inhibitor 10 | Potent, selective, and orally bioavailable ASK1 inhibitor | €130.00 | |
3997 | ASN-002 | Potent dual inhibitor of SYK and pan-JAK kinases | Inquire | |
2166 | AT 13148 dihydrochloride | ATP-competitive inhibitor of multi-AGC kinases | €70.00 | |
1539 | AT 7519 mesylate | CDK inhibitor | €80.00 | |
2219 | AT 9283 | Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl) | €85.00 | |
1597 | Aurora A inhibitor I | Aurora A inhibitor | €125.00 | |
1630 | Aurora A inhibitor II | Aurora A inhibitor | €125.00 | |
2345 | AZ 20 | Potent, orally active and selective inhibitor of ATR protein kinase | €105.00 | |
1545 | AZ 628 | B-Raf and C-Raf protein kinase inhibitor | €80.00 |