MAPK/ERK


The mitogen-activated protein kinase (MAPK) is a highly conserved family of serine/threonine kinases that mediate a board range of cellular processes, including proliferation, differentiation, motility, migration, stress response, apoptosis and survival. The activation of MAPK involves signaling pathways consisting of MAPK kinase (i.e. MAPKKK or MEKK) that activates MAPK/ERK (i.e. MAPKK or MEK). A variety of extracellular signals such as mitogens, cytokines, growth factors, and environmental stressors stimulate a phosphorylation-dependent increase in the activity of MAPK.
Activated MAPKs transduce the phosphorylation and activation of MAPK-activated protein kinases (MAPKAPKs), e.g. RSK, MSK, or MNK family, and MK2/3/5. There are three main MAPK families, signal-regulated kinase 1 and 2 (Erk1/2 or p44/42), the c-Jun N-terminal kinases 1-3 (JNK1-3)/ stress activated protein kinases (SAPK1A, 1B, 1C), the p38 isoforms (p38α, β, γ, and δ). ERK signaling is involved in cell division, migration and survival. p38 MAPK and JNK/SAPK pathways are activated by cellular stress. The p38 MAPK pathway regulates cell motility, transcription, and chromatin remodeling. JNK/SAPK signaling affects apoptosis and inflammation. Dysregulation of MAPK pathway results in tumorgenesis and other pathological conditions.
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B5820 RO5126766(CH5126766)Summary: Raf/MEK dual inhibitor -
A8716 LY3009120Target: RafSummary: pan-RAF and RAF dimer inhibitor -
B5867 SCH772984 TFASummary: ERK1/2 inhibitor -
B5866 SCH772984 HClSummary: ERK1/2 inhibitor -
B5942 AS601245Summary: c-Jun NH2-terminal protein kinase inhibitor -
B5960 PF-03394197(Oclacitinib)Summary: Novel Janus kinase inhibitor -
B6012 Pexmetinib (ARRY-614)Target: p38|Tie-2Summary: dual inhibitor of p38 MAPK and Tie2/Tek receptor tyrosine kinase -
B6014 BI-847325Summary: dual inhibitor of MEK and Aurora kinases -
B6024 DEL-22379Summary: inhibitor of the dimerization of ERK -
A9925 p-Cresyl sulfate potassiumSummary: A potassium form of p-Cresyl sulfate that acts as a pro-inflammatory agent

