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 (267)
Related Products (267)
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Antibodies (1)
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PARP1/ERK IN-1
0 ImagesCat. No.: HY-181842PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer.
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Multitarget AD-IN-8
0 ImagesCat. No.: HY-189262Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.
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Peptide R54
0 ImagesCat. No.: HY-P11011CAS No.: 2232233-39-3Synonyms: Pep R54; CXCR4 antagonist peptide 19
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NS-417 free base
0 ImagesCat. No.: HY-182401CAS No.: 160753-58-2NS-417 free base is an ERK1, ERK2, and Akt kinase activator with neuroprotective, neurite outgrowth potentiating, and dopaminergic cell population enhancing activity. NS-417 free base enhances activation of ERK1, ERK2, and Akt kinase via growth factor stimulation. NS-417 free base rescues cells from growth factor withdrawal-induced death, stimulates neurite outgrowth, increases tyrosine hydroxylase-positive cell counts, and displays neurotrophic-like activity in in vitro models. NS-417 free base can be used for the research of parkinson’s disease.
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Chalcomoracin
0 ImagesCat. No.: HY-N20674CAS No.: 76472-89-4Chalcomoracin is an orally active anticancer agent. Chalcomoracin exhibits anticancer, antibacterial, and α-glucosidase inhibitory activities, with an IC50 of 14.23 µM against yeast α-glucosidase and an IC50 of 5.5 μM against FabI of Staphylococcus aureus. Chalcomoracin reduces the phosphorylation levels of ERK, JNK, and P38; enhances the phosphorylation level of ERK1/2; regulates the MAPK, mTOR, AKT, and p53 signaling pathways; upregulates the expression of Chop, Bip, PINK1, GRP78, and GADD153; and downregulates the expression of Alix. Chalcomoracin induces apoptosis (apoptosis), endoplasmic reticulum stress (endoplasmic reticulum stress), paraptosis (paraptosis), ROS production, mitophagy (mitophagy), and autophagy (autophagy); it inhibits cancer cell viability, colony-forming ability, migration, invasion, proliferation, tumorigenesis, fatty acid synthesis, S. aureus growth, vitreous-stimulated retinal cell activity, and cell cycle progression at the G0/G1 phase. Chalcomoracin can be used in research related to hepatocellular carcinoma, non-small cell lung cancer, triple-negative breast cancer, prostate cancer, proliferative vitreoretinopathy, pancreatic cancer, diabetes, and bacterial infections.
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Sonvuterkib
0 ImagesCat. No.: HY-177132CAS No.: 2890225-50-8Synonyms: WX001Sonvuterkib (WX001) is a potent and orally active extracellular signal-regulated kinases (ERK) inhibitor with IC50 values of 1.4, 0.54 nM for ERK1, ERK2, respectively. Sonvuterkib inhibits cell proliferation. Sonvuterkib shows anticancer activity.
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CW-10201
0 ImagesCat. No.: HY-189305CW-10201 is a KRASG12D and KRASG12V PROTAC degrader with DC50 values of 4.0 nM. CW-10201 induces ubiquitination and degradation of KRASG12D and KRASG12V. CW-10201 mildly inhibits pERK1/2. CW-10201 does not induce degradation of IKZF1 and GSPT1. CW-10201 exhibits anticancer activity against pancreatic cancer and colorectal cancer. CW-10201 can be used for research on pancreatic cancer and colorectal cancer.
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24-O-Acetyllycoclavanol
0 ImagesCat. No.: HY-N17131CAS No.: 13956-53-124-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum.
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M1/M4 muscarinic agonist 4
0 ImagesCat. No.: HY-187957M1/M4 muscarinic agonist 4 is a dual-site muscarinic acetylcholine receptor ligand with potent agonistic activity at M1/M4 muscarinic acetylcholine receptors. M1/M4 muscarinic agonist 4 activates M1R to induce phosphorylation of ERK1/2, and activates M4R to induce GαoB protein activation as well as ERK1/2 phosphorylation. M1/M4 muscarinic agonist 4 exhibits higher binding affinity for M4R than for other muscarinic receptors, while its binding affinity for the W435A mutant M4R is reduced. M1/M4 muscarinic agonist 4 can be used in the research of schizophrenia.
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Urocortin II, human TFA
0 ImagesCat. No.: HY-P1752AUrocortin II, human TFA is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human TFA has an effect of promoting satiet and neuroprotective effect. Urocortin II, human TFA also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human TFA can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human TFA can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human TFA can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.
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MAPK-IN-6
0 ImagesCat. No.: HY-180807MAPK-IN-6 is a blood-brain barrier-permeable MAPK inhibitor. MAPK-IN-6 inhibits oxidative stress-induced activation of the MAPK signaling cascade, including the phosphorylation of ERK1/2, p38 and JNK. MAPK-IN-6 eliminates intracellular reactive oxygen species (ROS) accumulation, stabilizes mitochondrial membrane potential and inhibits cell apoptosis. MAPK-IN-6 can be used for the research of ischemic stroke.
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NEPP11
0 ImagesCat. No.: HY-180327CAS No.: 313051-12-6NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.
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Anti-inflammatory agent 31
0 ImagesCat. No.: HY-150587CAS No.: 3051838-54-8Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
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Evariquinone
0 ImagesCat. No.: HY-118817CAS No.: 594860-23-8Evariquinone is an anthraquinone compound isolated from the endophytic fungus Colletotrichum sp. JS-0367 of mulberry. Evariquinone possesses direct antioxidant activity. It inhibits excessive phosphorylation of the JNK, ERK1/2 and p38 MAPK signaling pathways by suppressing ROS and Ca2+, thereby reducing neuronal apoptosis. Evariquinone can be used to study glutamate excitotoxicity-related neurological disorders (such as Alzheimer's disease, Parkinson's disease, cerebral ischemia, etc.).
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Leupeptin hemisulfate (Standard)
0 ImagesLeupeptin hemisulfate (Standard) is the analytical standard of Leupeptin hemisulfate (HY-18234A ). This product is intended for research and analytical applications. Leupeptin hemisulfate is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hemisulfate significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hemisulfate inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hemisulfate can be used in research on chronic inflammatory diseases and skin tumorigenesis.
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KRAS G12C-IN-78
0 ImagesCat. No.: HY-181965CAS No.: 3023465-20-2KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer.
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ERK1/2 inhibitor 10
0 ImagesCat. No.: HY-162460CAS No.: 3056077-07-4ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations.
