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.
-
BA2810 1A-116Summary: 1A-116 is an inhibitor specific for the W56 residue that effectively prevents the induced activation and blocks the interaction of the -
BA2812 ASK1-IN-1Summary: ASK1-IN-1 is a CNS permeant apoptosis signal-regulated kinase 1 (ASK1) inhibitor with good potency. -
BA2816 SSK1Summary: SSK1, a senescence-specific killing compound, is a β-galactosidase-targeting precursor that reduces inflammation. -
BA2865 KY-05009Summary: KY-05009 is an ATP-competitive inhibitor. -
BA2886 MBM-55Summary: MBM-55 is an effective inhibitor. -
BA2893 DMU-212Summary: DMU-212 is a resveratrol methylated derivative with antidisintegrative, antiproliferative, antioxidant and apoptosis-promoting activities. -
BA2894 ARS-853Summary: ARS-853 is a selective, covalent inhibitor. -
BA3657 AZD7624Summary: AZD7624 is an inhalable inhibitor. -
BA2003 U01263 CitationSummary: A potent, non-ATP-competitive, selective MEK inhibitor -
BA3877 TNG348Summary: TNG348 is an orally active deubiquitinating enzyme inhibitor.

