MAPK

Similar to the PI3K/AKT/mTOR pathway, the MAPK/Erk signaling cascade is activated by a wide variety of receptors involved in growth and differentiation including receptor tyrosine kinases (RTKs), integrins, ion channels, and extracellular stimuli such as heat and stress. The specific components of the cascade vary greatly among different stimuli, but the architecture of the pathway usually includes a set of adaptors (e.g. Shc, GRB2, Crk, etc.) linking the receptor to a guanine nucleotide exchange factor (SOS, C3G, etc.) transducing the signal to small GTP binding proteins (Ras, Rap1), which in turn activate the core unit of the cascade composed of a MAPKKK (Raf), a MAPKK (MEK1/2), and MAPK (Erk: extracellular signal-regulated kinases). An activated Erk dimer can regulate targets in the cytosol and also translocate to the nucleus where it phosphorylates a variety of transcription factors regulating gene expression[1],[2]. One example of the most recent additions to this class of compounds is FMK (Axon 1848), a potent, highly specific and irreversible inhibitor of p90 ribosomal protein S6 kinase RSK1 and RSK2. This drug is capable of inducing significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells[3]. Actually, MEK enzymes are members of the class of dual specificity mitogen-activated protein kinase kinase (EC 2.7.12.2) and should not be listed within the section of serine/threonine specific kinases (EC 2.7.11.). However, as they are integral members of the group of enzymes involved in MAPK/ERK signaling, and besides having the capability to phosphorylate tyrosine residues, they are also capable of phosphorylating serine/threonine sites of substrates, MEK inhibitors are listed in this section for kinases involved in the MAPK/ERK signaling pathway.


[1] Regulatory mechanisms of mitogen-activated kinase signaling. Zhang Y, Dong C. Cell Mol Life Sci. 2007, 64, 2771-2789.
[2] Pathological roles of MAPK signaling pathways in human diseases. Kim EK, Choi EJ. Biochim Biophys Acta. 2010, 1802, 396-405.
[3] Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Cohen MS, Zhang C, Shokat KM,Taunton J. Science 2005, 308 1318-1321.

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Axon ID Name Description From price
2552 Adjudin Non-hormonal male contraceptive with anti-proliferative activity €125.00
1291 AEG 3482 JNK inhibitor €85.00
2389 AICAR Potent AMPK activator and inducer of differentiation of NSCs €45.00
2611 APS-2-79 Inhibitor of KSR and oncogenic Ras signaling €90.00
2002 AS 602801 JNK inhibitor, which inhibited JNK1, JNK2 and JNK3 €120.00
2179 ASK1 Inhibitor 10 Potent, selective, and orally bioavailable ASK1 inhibitor €125.00
5051 Axon Ligands™ Cell signaling and Oncology compound library Axon Ligands™ Cell signaling and Oncology compound library Inquire
5053 Axon Ligands™ Stem cell compound library Axon Ligands™ Stem cell compound library Inquire
1545 AZ 628 B-Raf and C-Raf protein kinase inhibitor €80.00
1516 AZD 6244 MEK1 and MEK2 inhibitor €70.00
1999 AZD 8330 MEK 1 inhibitor €105.00
2178 BCI Allosteric inhibitor of dual-specificity phosphatases (DUSP) €75.00
1528 BI-D1870 RSK inhibitor (p90 RSK specific) €80.00
1358 BIRB 796 MAPK inhibitor (p38 specific) €70.00
1808 BIX 02188 MEK5 inhibitor; ERK5 inhibitor €125.00

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