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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C4949 SB 202474Summary: a negative control in studies of p38 inhibition -
B7850 BMS-582949 hydrochlorideSummary: p38 MAPK inhibitor -
C5545 MK2 Inhibitor IVTarget: MK2Summary: highly selective, non-ATP competitive MK2 inhibitor -
C5316 RWJ 67657Summary: orally active inhibitor of the MAP kinases p38α and p38β -
C5489 8-CPT-Cyclic AMP (sodium salt)Summary: lipophilic activator of the cyclic-AMP- and cyclic-GMP-dependent protein kinases, PKA and PKG -
B1172 B-Raf inhibitor 1Summary: Potent and selective B-Raf inhibitor -
B1173 B-Raf inhibitor 1 dihydrochlorideSummary: B-Raf inhibitor,potent and selective -
B1407 Dabrafenib (GSK2118436)3 CitationTarget: RafSummary: Inhibitor of BRAF(V600) mutants -
B1267 RefametinibTarget: MEKSummary: MEK 1/ MEK 2 inhibitor -
B1174 LGX818Target: RafSummary: RAF inhibitor,potent and selective

