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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A8308 PH-7978041 CitationSummary: P38 MAP kinase inhibitor, potent and selective -
A8313 RAF265Target: Raf|VEGFRSummary: Multiple intracellular kinases inhibitor -
A8371 AZ 628Summary: Raf kinases,potent and ATP-competitive -
A8374 AZD8330Target: MEKSummary: MEK 1/2 inhibitor -
A8435 FurosemideTarget: Na /K /Cl- Symporters (NKCCs)|GABAA ReceptorsSummary: GABAA receptors antagonist -
A8545 ZM336372Summary: C-Raf inhibitor, potent and selective -
A8686 VX-745Target: p38Summary: P38α inhibitor,highly potent and selective -
A8687 VX-702Summary: P38α MAPK inhibitor,highly selective and ATP-competitive -
A8688 TAK-715Summary: p38 MAPK inhibitor -
A8689 PD 169316Target: p38Summary: P38 MAPK inhibitor

