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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B3261 RO4987655Summary: MEK inhibitor -
B3275 TCS JNK 5aTarget: JNKSummary: JNK2 and JNK3 inhibitor -
B1285 SB 203580 hydrochlorideTarget: p38Summary: Specific p38-MAPKs inhibitor -
B2227 BI-D18701 CitationTarget: p90 S6KSummary: P90 RSK inhibitor,ATP-competitive and cell-permeable -
B1405 GW50742 CitationSummary: C-Raf inhibitor,potent and selective -
B1406 SB5908851 CitationSummary: Potent B-Raf inhibitor -
B1260 CC-401Summary: JNK inhibitor,ATP-competitive -
B1621 TAK-733Target: MEKSummary: MEK allosteric site inhibitor -
B6159 Vacquinol-1Summary: MAPK kinase 4 (MKK4) activator -
B6177 PLX7904Summary: paradox-breaker RAF inhibitor, potent and selective

