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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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.
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Pheophytin a
0 ImagesPheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease.
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Polfurmetinib
0 ImagesSynonyms: MEK-IN-6
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Quin-C7
0 ImagesQuin-C7 is an orally active FPR2/ALX antagonist. Quin-C7 binds to the orthosteric ligand-binding pocket of FPR2/ALX, modulates receptor activation, and inhibits pro-inflammatory ERK signaling mediated by serum amyloid A (SAA). Quin-C7 reduces pro-inflammatory mediators TNF-α levels, increases anti-inflammatory IL-10, decreases inflammatory neutrophils and pro-inflammatory M1 macrophages, downregulates ERK1/2 phosphorylation, and upregulates JNK1/2/3 phosphorylation. Quin-C7 blocks FPR2/mFpr2 signaling, reduces brain lesion volume. Quin-C7 can be used for the research of inflammatory bowel disease and neuromyelitis optica spectrum disorder.
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TCB-32 hydrochloride
0 ImagesCat. No.: HY-176862ACAS No.: 169764-95-8TCB-32 (Compound I-1) hydrochloride is a FGFR1 agonist with an EC50 of 0.88 μM. TCB-32 hydrochloride significantly increases cell proliferation through activating FGFR1 signaling pathway as bFGF and its downstream ERK1/2 with excellent thermal stability. TCB-32 hydrochloride can replace bFGF in serum-free cell culture media. TCB-32 hydrochloride can be used for tissue repair and wound healing related diseases like psoriasis and eczema research.
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Sophoranone
0 ImagesSynonyms: (-)-Sophoranone; SophoranonSophoranone ((-)-Sophoranone; Sophoranon) is an orally active competitive inhibitor of CYP2C9 (IC50 = 0.966 μM) and CYP3A4. Sophoranone is a prenylated flavonoid isolated from the roots of Sophora subprostrata. Sophoranone induces apoptosis by increasing reactive oxygen species (ROS) and opening the mitochondrial channel, while upregulating myogenic genes to promote muscle regeneration. Sophoranone can be used for research on asthma, leukemia, and paralytic strabismus.
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Pizotifen
0 ImagesSynonyms: Pizotyline; BC-105Pizotifen (Pizotyline) is a 5-HT2 receptor antagonist. Pizotifen inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.
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Ombuoside
0 ImagesOmbuoside has antioxidant properties, inhibiting ROS production and apoptosis. Ombuoside exerts neuroprotective effects through the ERK-JNK-caspase-3 system. Ombuoside promotes Dopamine biosynthesis through TH and CREB activation. Ombuoside exhibits antimicrobial activity against several Gram-positive and Gram-negative bacteria, as well as Candida albicans
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Urocortin II, human acetate
0 ImagesCat. No.: HY-P1752BPurity: 99.50%Urocortin II, human acetate is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human acetate has an effect of promoting satiet and neuroprotective effect. Urocortin II, human acetate also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human acetate can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human acetate can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human acetate can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.
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Ganglioside GT1b (bovine) ammonium
0 ImagesGanglioside GT1b (bovine) ammonium is a member of the ganglioside family. Ganglioside GT1b (bovine) ammonium acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b (bovine) ammonium induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b (bovine) ammonium enhances porcine oocyte maturation and induce activation of EGFR and ERK1/2 signaling. Ganglioside GT1b (bovine) ammonium is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b (bovine) ammonium can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease.
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EXP3179
0 ImagesSynonyms: Losartan Carboxaldehyde; DuP 167EXP3179 (Losartan Carboxaldehyde) is a metabolite of Losartan (HY-17512). EXP3179 binds to AT1R with an affinity of 20 nM and blocks ANGII-induced AT1R signaling, inhibiting ERK1/2 activation. EXP3179 reduces NADPH oxidase activity. EXP3179 inhibits Phenylephrine (HY-B0769)-induced aortic contraction through an endothelium-dependent, NO-dependent mechanism. EXP3179 dose-dependently inhibits type I collagen-induced platelet aggregation and activation through GPVI binding, reducing platelet adhesion to the injured site. EXP3179 lowers blood pressure in normotensive and spontaneously hypertensive rats and mice. EXP3179 can be used for research on type 2 diabetes, hypertensive heart disease, hypertension, thrombosis, and coronary artery disease.
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Cucurbitacin IIa
0 ImagesSynonyms: Hemslecin ACucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC50 of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.
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SHR2415
0 ImagesSHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer.
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Physalin B
0 ImagesCat. No.: HY-N7695CAS No.: 23133-56-4Physalin B is an orally active anti-inflammatory and anticancer agent. Physalin B can be isolated from Physalis alkekengi L. var. Franchetii. Physalin B inhibits the activation of the NF-κB, NLRP3 inflammasome, STAT3, PI3K/Akt and Hedgehog signaling pathways, regulates the phosphorylation levels of GSK-3β, p38 MAPK, ERK1/2 and JNK, and promotes the nuclear translocation of NRF2. Physalin B reduces the levels of pro-inflammatory cytokines and factors, induces mitochondrial reactive oxygen species (mito-ROS) production, Apoptosis, G2/M cell cycle arrest and incomplete Autophagy, alters cytoskeleton structure and alleviates oxidative stress. Physalin B reduces cancer cell viability, ameliorates liver and lung tissue damage and alleviates liver fibrosis. Physalin B can be used in research related to ulcerative colitis, breast cancer, acute lung injury, colon cancer, non-alcoholic steatohepatitis, liver fibrosis, lung cancer, pancreatic cancer, lymphoma, ovarian cancer, sarcoma and leukemia.
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Gestodene
0 ImagesSynonyms: SHB 331; WL 70Gestodene (SHB 331; WL 70) is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.
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Erlotinib Hydrochloride (Standard)
0 ImagesSynonyms: CP-358774 hydrochloride (Standard); NSC 718781 hydrochloride (Standard); OSI-774 hydrochloride (Standard)Erlotinib Hydrochloride Standard (CP-358774 hydrochloride Standard) is the analytical standard of Erlotinib Hydrochloride (HY-12008). This product is intended for research and analytical applications. Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride 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 Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride 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 Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride 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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Pizotifen malate
0 ImagesPizotifen malate (Pizotyline malate) is a 5-HT2 receptor antagonist. Pizotifen malate inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen malate causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen malate blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen malate exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen malate exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen malate can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.
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SKLB-D18
0 ImagesCat. No.: HY-173119Purity: 98.06%SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC50 of 38.69 nM and a Kd of 126.9 nM against human ERK1, an IC50 of 40.12 nM and a Kd of 209.8 nM against ERK2, and an IC50 of 59.72 nM and a Kd of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer.
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N-Feruloylserotonin
0 ImagesSynonyms: (E/Z)-MoschamineN-Feruloylserotonin ((E/Z)-Moschamine) is a serotonin hydroxycinnamic acid amide. It can be isolated from a variety of plants, particularly the seeds of safflower (Carthamus tinctorius L.). N-Feruloylserotonin inhibits KCl- and 5-HT-induced elevation of intracellular [Ca2+]i. It suppresses PDGF-BB-induced phosphorylation of PDGFRβ and ERK1/2. N-Feruloylserotonin exerts anti-inflammatory effects on aortic endothelial cells. It inhibits atherosclerotic plaque formation in apolipoprotein E-deficient mice.
