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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BA2003 U01263 CitationSummary: A potent, non-ATP-competitive, selective MEK inhibitor -
BA3877 TNG348Summary: TNG348 is an orally active deubiquitinating enzyme inhibitor. -
BA4406 PERK-IN-2Summary: PERK-IN-2 is a potent inhibitor. -
BA4410 Takeda-6DSummary: Takeda-6D is an orally effective inhibitor at 7.0 and 2.2 nM, respectively. -
BA4439 BilobetinSummary: Bilobetin is an active ingredient that lowers blood lipids and improves insulin action. -
BA4637 IMM-H007Summary: IMM-H007 (WS070117) is an orally effective (AMP-activated protein kinase) activator and (transforming growth factor beta 1) antagonist. -
BA7032 MoringinSummary: Moringin is a potent and selective natural agonist of ion channels. -
BA6105 MSU-42011Summary: MSU-42011 is an orally active retinoid X receptor agonist. -
BA6439 BIX02188Summary: BIX02188 is a potent and selective inhibitor. -
BA6445 α-AmyrinSummary: α-Amyrin is a pentacyclic triterpenoid with oral activity.

