ERK2
ERK2 (MAPK1) is a core effector kinase of the Ras/Raf/MEK/ERK signaling cascade and functions as an integration point for extracellular signals that regulate cell proliferation, differentiation, survival, transcriptional programs, and development[1][2]. Mechanistically, ERK2 is activated through MEK-dependent phosphorylation and subsequently phosphorylates numerous substrates across cellular compartments, linking growth factor stimulation to broad biological responses[3]. Because ERK signaling controls fundamental cellular processes, dysregulation of the pathway is associated with multiple pathological conditions, particularly tumorigenesis, and aberrant ERK pathway activity is observed in a substantial proportion of human cancers[4]. In experimental systems, genetic disruption studies demonstrate that ERK2 is essential for normal mammalian development, as loss of ERK2 causes embryonic lethality, highlighting the critical requirement for adequate ERK signaling output[3]. Compared with the closely related isoform ERK1 (MAPK3), ERK2 shares highly conserved activation mechanisms, substrate recognition properties, and signaling functions, and many studies support the view that biological outcomes are largely determined by total ERK activity rather than strict isoform-specific functions[3]. For experimental applications, ERK pathway inhibitors targeting RAF, MEK, or ERK have been extensively developed and are widely used to investigate ERK-dependent signaling networks, disease mechanisms, therapeutic resistance, and pathway regulation in cancer models[4][5].
References:
- [1]. Mitogen Activated Protein Kinase 1. Sciencedirect topic.
- [2]. Wikipedia.
- [3]. Buscà R, et al. ERK1 and ERK2 Map Kinases: Specific Roles or Functional Redundancy? Front Cell Dev Biol. 2016 Jun 8;4:53. [Content Brief]
- [4]. Timofeev O, et al. ERK pathway agonism for cancer therapy: evidence, insights, and a target discovery framework. NPJ Precis Oncol. 2024 Mar 14;8(1):70. [Content Brief]
- [5]. Sah VK, et al. Advances in ERK1/2 inhibition: a medicinal chemistry perspective on structure and regulation. J Enzyme Inhib Med Chem. 2025 Dec;40(1):2555510. [Content Brief]
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ERK2 Related Products (254)
Related Products (254)
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Antibodies (1)
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Chondroitin sulfate (from chicken)
0 ImagesSynonyms: Chondroitin polysulfate (from chicken)Chondroitin sulfate (from chicken) (Chondroitin polysulfate (from chicken)) is an orally active, sulfated linear polysaccharide extracted from chickens, which belongs to glycosaminoglycans. Chondroitin sulfate (from chicken) reduces the phosphorylation levels of ERK1/2 and p38MAPK, inhibits the expression of inflammatory cytokines and MMP, and downregulates the levels of IL-1β, IL-6, TNF-α and PGE2. Chondroitin sulfate (from chicken) improves motor function, protects cartilage tissue, reverses chondrocyte aggregation, and regulates the structure of intestinal flora. Chondroitin sulfate (from chicken) can be used in research related to osteoarthritis.
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UNC1062
0 ImagesUNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.
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Trimebutine
0 ImagesTrimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
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Zoniporide hydrochloride hydrate
0 ImagesSynonyms: CP-597396 hydrochloride hydrateZoniporide hydrochloride hydrate (CP-597396 hydrochloride hydrate) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride hydrate reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride hydrate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.
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N-(p-Coumaroyl) Serotonin
0 ImagesN-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.
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Trimebutine maleate
0 ImagesTrimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
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Secretoneurin, rat
0 ImagesSecretoneurin, rat is a 33-amino acid neuropeptide produced by proteolytic processing of chromogranin II, widely distributed in the central and peripheral nervous systems, and its release is calcium-dependent. Secretoneurin, rat modulates the activities of caspase-3, caspase-1, the NLRP3 inflammasome, IGF-1R, VEGFR1, VEGFR2, FGFR3, AMPK, ERK1/2/MAPK, and Jak2/Stat3 pathways. Secretoneurin, rat regulates neuronal apoptosis, synaptic structure, inflammation, neurogenesis, angiogenesis, oxidative stress, cardiomyocyte hypertrophy, dopamine release, and cell migration and proliferation. Secretoneurin, rat is used in studies of global cerebral ischemia, myocardial infarction, stroke, and cardiac hypertrophy.
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4-Methylbenzylidene camphor
0 ImagesSynonyms: 4-MBC; Enzacamene4-Methylbenzylidene camphor (4-MBC) is an endocrine disrupter that produces estrogen-like effects. 4-Methylbenzylidene camphor decreases the proliferation of human trophoblast cells and induces apoptosis. 4-Methylbenzylidene camphor activates PI3K/AKT and ERK1/2 signaling pathways and elevates intracellular ROS production. 4-Methylbenzylidene camphor is a ultraviolet (UV) filter and may hamper normal placental formation during early pregnancy.
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Armepavine
0 ImagesArmepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia.
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Rineterkib
0 ImagesRineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.
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FZ1 peptide
0 ImagesCat. No.: HY-P11474Purity: 99.92%FZ1 peptide is a cyclic heptapeptide and also an integrin αvβ3 agonist. FZ1 peptide activates the FAK/PI3K-AKT/ERK pathway and upregulates VEGFC to promote angiogenesis. FZ1 peptide exhibits antibacterial activity in extracts of HA-c-FZ1 hydrogel; it inhibits LPS-induced proinflammatory cytokine secretion in RAW264.7 macrophages; it reduces H2O2-induced ROS levels; it increases the healing rate of scratch wounds. FZ1 peptide can be used in studies related to diabetic skin wounds.
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ML191
0 ImagesSynonyms: CID23612552ML191 (CID23612552) is a GPR55 antagonist. ML191 inhibits ERK phosphorylation and PKC β II translocation downstream of GPR55 signaling. ML191 suppresses LPI-induced activation of ERK1/2 and p38 MAPK signaling, blocks the transcription of RANKL-induced osteoclastogenesis markers, and reduces the bone resorption activity of mature osteoclasts promoted by RANKL. ML191 can be used to investigate diseases associated with bone degradation caused by excessive osteoclast activation, such as osteoporosis and bone damage during the formation stage of bone metastases.
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Fulipiftide
0 ImagesSynonyms: PSP 29-mer, anti-inflammatory peptideFulipiftide (PSP 29-mer) is a short peptide derived from pigment epithelium-derived factor (PEDF). Fulipiftide induces the phosphorylation of ERK2 and STAT3, enriches tendon stem/progenitor cell markers, maintains cell stemness, promotes colony formation and niche expansion, and drives cell infiltration into injured tendons. Fulipiftide promotes the oriented formation of collagen fibers, regulates collagen deposition, and reduces inflammatory cell infiltration and neovascularization. Fulipiftide can be used in studies related to acute tendon injury.
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Eras-4001
0 ImagesEras-4001 is a potent, orally active pan-KRAS inhibitor with Kd values of 110, 13 and 39 pM against wild-type, G12D and G12V mutant KRAS, respectively, and exhibits selectivity toward wild-type HRAS and NRAS. Eras-4001 inhibits ERK1/2 phosphorylation and cell viability in cancer cells. Eras-4001 induces tumor growth inhibition and regression in subcutaneous xenograft models. Eras-4001 can be used in research on non-small cell lung cancer, ovarian cancer, etc.
