1. Signaling Pathways
  2. MAPK/ERK Pathway
    Stem Cell/Wnt
  3. ERK

ERK

Extracellular signal regulated kinases

ERKs (Extracellular-signal-regulated kinases) are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. Many different stimuli, including growth factors, cytokines, virus infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens, activate the ERK pathway. In the MAPK/ERK pathway, Ras activates c-Raf, followed by mitogen-activated protein kinase kinase (abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below). Ras is typically activated by growth hormones through receptor tyrosine kinases and GRB2/SOS, but may also receive other signals. ERKs are known to activate many transcription factors, such as ELK1, and some downstream protein kinases. Disruption of the ERK pathway is common in cancers, especially Ras, c-Raf and receptors such as HER2.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12764R
    6-OAU (Standard)
    Inhibitor
    Prochloraz manganese (Standard) is the analytical standard of Prochloraz manganese. This product is intended for research and analytical applications. Prochloraz manganese is an antifungal agent, and is used in agricultural industries.
    6-OAU (Standard)
  • HY-P10833
    C-VGB3
    Inhibitor
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-P3963
    Thymus Factor
    Inhibitor
    Thymus Factor (Thymulin) is a key factor responsible for the maturation of humoral immunological faculty. Thymulin is an inhibitor of ERK.
    Thymus Factor
  • HY-175288
    αMβ2 integrin agonist-1
    Activator
    αMβ2 integrin agonist-1 (Compound 8) is a highly selective αMβ2 integrin agonist with anti-inflammatory activity (EC50=1.4 nM). αMβ2 integrin agonist-1 activates integrin-mediated cell adhesion and JNK/ERK signaling. αMβ2 integrin agonist-1 induces tumor-associated macrophage repolarization and enhances antitumor T-cell immune responses. αMβ2 integrin agonist-1 is promising for research of cancers and chronic inflammatory diseases (e.g., pancreatic cancer, rheumatoid arthritis).
    αMβ2 integrin agonist-1
  • HY-169412
    MAPK-IN-3
    Activator
    MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.
    MAPK-IN-3
  • HY-174415
    ZSH-2117
    Inhibitor
    ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFRL858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFRL858R/T790M/C797S xenograft mice model. Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
    ZSH-2117
  • HY-135564
    RK-682 hemicalcium
    Inhibitor
    RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].
    RK-682 hemicalcium
  • HY-175286
    α4β1 antagonist-1
    Inhibitor
    α4β1 antagonist-1 (Compound 4) is a highly selective α4β1 integrin antagonist (IC50=15 nM). α4β1 antagonist-1 inhibits integrin-mediated cell adhesion and ERK1/2 signaling activation. α4β1 antagonist-1 also exhibits partial agonism toward αMβ2 integrin (EC50=23 nM). α4β1 antagonist-1 is promising for research of chronic inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis) and cancers.
    α4β1 antagonist-1
  • HY-122019
    ABD56
    ABD56 is a compound that induces osteoclast apoptosis and has the activity of inhibiting osteoclast formation and inducing apoptosis. ABD56 can inhibit osteoclast formation and induce apoptosis, and its mechanism is related to the inhibition of NFκB and ERK pathways.
    ABD56
  • HY-112363
    Aloisine A
    Inhibitor
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
    Aloisine A
  • HY-P3206
    Serum thymic factor
    Inhibitor 98.09%
    Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases.
    Serum thymic factor
  • HY-151430
    Nrf2/HO-1 activator 1
    Inducer
    Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator, neuroprotective agent. Nrf2/HO-1 activator 1 shows neuroprotective and antioxidant activities. Nrf2/HO-1 activator 1 can be used in Parkinson's disease (PD) research.
    Nrf2/HO-1 activator 1
  • HY-164350
    KRAS inhibitor-27
    Inhibitor
    KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway.
    KRAS inhibitor-27
  • HY-N12561
    Pestanoid A
    Inhibitor
    Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis.
    Pestanoid A
  • HY-172110
    Apoptosis inducer 35
    Inhibitor
    Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis.
    Apoptosis inducer 35
  • HY-P10421
    PKCδ substrate
    Modulator
    PKCδ substrate acts as a nuclear transporter of ERK2 and is involved in ERK2 mediated gene activation. PKCδ is involved in the regulation of cell growth, proliferation, cell cycle arrest, and apoptosis by phosphorylating hBVR and other proteins. PKCδ substrate can be used to study the development of diseases, especially cancer biology.
    PKCδ substrate
  • HY-150687
    ZINC12409120
    Inhibitor
    ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM.
    ZINC12409120
  • HY-171656
    G721-0282
    Inhibitor
    G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
    G721-0282
  • HY-N0590R
    Corynoxeine (Standard)
    Inhibitor
    Corynoxeine (Standard) is the analytical standard of Corynoxeine. This product is intended for research and analytical applications. Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.
    Corynoxeine (Standard)
  • HY-162850
    DOR agonist 2
    Activator
    DOR agonist 2 (Compound 3) is a Delta Opioid Receptor agonist. DOR agonist 2 can inhibit the expression of TNF-α, prevent NF-κB transport to the nucleus, and activate the G protein-mediated ERK1/2 pathway. DOR agonist 2 can be used in the study of neurodegenerative diseases.
    DOR agonist 2
Cat. No. Product Name / Synonyms Application Reactivity

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