ERK1
ERK1 (MAPK3) is a serine/threonine protein kinase that functions as an essential effector of the MAPK/ERK signaling cascade and transduces extracellular signals controlling cell proliferation, differentiation, migration, and survival[1][2]. Mechanistically, ERK1 operates downstream of the Ras/Raf/MEK pathway, where dual phosphorylation activates ERK signaling and enables phosphorylation of numerous substrates across multiple cellular compartments, thereby regulating gene expression and diverse physiological processes[2]. Because the MAPK/ERK pathway integrates growth factor, hormone, and stress-associated signals, dysregulated ERK signaling contributes to pathological conditions including cancer and other diseases characterized by aberrant cellular proliferation and survival signaling[1]. In experimental systems, ERK1 has been extensively investigated in developmental, vascular, and disease models to define its contribution to signal transduction and tissue responses[2][3]. Compared with the closely related isoform ERK2 (MAPK1), ERK1 exhibits highly conserved activation mechanisms, substrate recognition properties, and signaling outputs, and current evidence generally supports substantial functional redundancy between the two kinases[2]. Nevertheless, isoform-specific studies have identified distinct biological contexts in which ERK1 and ERK2 contribute differently to physiological processes, including vascular remodeling and arteriogenesis, indicating that isoform-dependent functions can emerge in specific cellular environments[3]. For experimental applications, pharmacological ERK1/2 inhibitors are widely used to interrogate terminal MAPK pathway signaling and to investigate mechanisms of therapeutic resistance associated with reactivation of ERK signaling downstream of RAF or MEK inhibition[1].
References:
- [1]. 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]
- [2]. 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]
- [3]. Ricard N, et al. Isoform-Specific Roles of ERK1 and ERK2 in Arteriogenesis. Cells. 2019 Dec 21;9(1):38. [Content Brief]
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ERK1 Related Products (233)
Related Products (233)
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Antibodies (7)
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Erlotinib-d8
0 ImagesCat. No.: HY-50896S3CAS No.: 1266656-97-6Synonyms: CP-358774-d8; NSC 718781-d8; OSI-774-d8Erlotinib-d8 (CP-358774-d8) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.
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Famotidine-13C
0 ImagesCat. No.: HY-B0377S1Synonyms: MK-208-13CFamotidine-13C (MK-208-13C) is the 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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CP-724714 succinate
0 ImagesCat. No.: HY-14674ACAS No.: 543681-31-8CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.
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Methyl helicterate
0 ImagesCat. No.: HY-125522CAS No.: 102637-02-5Methyl helicterate is a triterpenoid, that can be isolated from Helicteres angustifolia (Sterculiaceae). Methyl helicterate inhibits hepatic stellate cell activation and promotes cell apoptosis through downregulating the ERK1/2 signaling pathway.
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Norflurazon (Standard)
0 ImagesCat. No.: HY-114849RCAS No.: 27314-13-2Synonyms: SAN 9789 (Standard)Norflurazon (Standard) (SAN 9789 (Standard)) is the analytical standard of Norflurazon (HY-114849). This product is intended for research and analytical applications. Norflurazon (SAN 9789) is a pre-emergence Herbicide. Norflurazon non-competitively inhibits phytoene desaturase by competing with the enzyme cofactor and disrupts carotenoid biosynthesis, thereby leading to chlorophyll photodegradation and chlorosis. Norflurazon inhibits MGDG synthase, CDP-choline phosphotransferase, Omega-3 FAD7 desaturase, and PG delta-3-trans desaturase, and activates LysoPC-acyltransferase and Omega-3 FAD3 desaturase. Norflurazon inhibits photosynthetic membrane organization, mitochondrial respiration, ATP production, PI3K signaling, and ERK1/2 phosphorylation. Norflurazon activates MAPK P38 phosphorylation and ER stress signaling. Norflurazon induces morphological malformations and cardiovascular effects in zebrafish embryos.
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Erlotinib mesylate
0 ImagesCat. No.: HY-12008ACAS No.: 248594-19-6Synonyms: CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylateErlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.
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Trimebutine (Standard)
0 ImagesTrimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine 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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Erlotinib-d4
0 ImagesCat. No.: HY-50896S2CAS No.: 1130852-41-3Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.
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MptpB-IN-3
0 ImagesCat. No.: HY-183688CAS No.: 3104354-58-4MptpB-IN-3 is a selective inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC50 of 0.19 μM. MptpB-IN-3 blocks MptpB-mediated inhibition of the macrophage MAPK pathway and restores the phosphorylation levels of Erk1/2 and p38. MptpB-IN-3 exhibits direct anti-tuberculosis activity against Mycobacterium tuberculosis and reduces the Mycobacterium tuberculosis load in mouse macrophages. MptpB-IN-3 can be used for tuberculosis research.
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Berkeleyacetal C
0 ImagesCat. No.: HY-N10175CAS No.: 959772-67-9keleyacetal C, a meroterpenoid compound with anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways. Berkeleyacetal C significantly inhibits the expression of iNOS and the following NO production by macrophages. Berkeleyacetal C inhibits expression and secretion of key pro-inflammatory factors and chemokines (TNF-α, IL-6, IL-1β, MIP-1α, and MCP-1). Berkeleyacetal C also inhibits activation of neutrophils and reactive oxygen species (ROS) production. Berkeleyacetal C can be used for the study of inflammatory disorders.
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Cavidine
0 ImagesCat. No.: HY-101546ACAS No.: 32728-75-9Synonyms: (+)-CavidineCavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain.
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2"-O-Galloylhyperin (Standard)
0 ImagesCat. No.: HY-N0526RCAS No.: 53209-27-12"-O-Galloylhyperin (Standard) is the analytical standard of 2"-O-Galloylhyperin (HY-N0526). This product is intended for research and analytical applications. 2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease.
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ADA-07
0 ImagesCat. No.: HY-122859CAS No.: 2252153-94-7ADA-07 is a TOPK inhibitor with activity at the ATP-binding pocket that does not inhibit MEK1 activity. ADA-07 suppresses solar ultraviolet (SUV)-induced phosphorylation of ERK1/2, p38, and JNKs, and inhibits AP-1 activity. ADA-07 attenuates tumor incidence, multiplicity, and volume in SUV-exposed SKH-1 hairless mice. ADA-07 can be used for the research of solar ultraviolet-induced skin carcinogenesis.
