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-181350
    CAIX/XII/NAMPT-IN-1
    Inhibitor
    CAIX/XII/NAMPT-IN-1 is a triple inhibitor of carbonic anhydrase IX/XII and nicotinamide phosphoribosyltransferase (NAMPT) with a hCA IX Ki of 78.1 nM, hCA XII Ki of 64.4 nM, and hNAMPT IC50 of 168 nM. CAIX/XII/NAMPT-IN-1 induces apoptosis, ROS accumulation, suppresses ERK/AKT signaling, inhibits DNA synthesis, and causes mitochondrial dysfunction. CAIX/XII/NAMPT-IN-1 exerts antiproliferative effects against multiple cancer cells under normoxic and hypoxic conditions. CAIX/XII/NAMPT-IN-1 can be used for the research of cancer, such as renal carcinoma, glioblastoma and colorectal cancer.
    CAIX/XII/NAMPT-IN-1
  • 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
  • HY-B0185AS1
    Lidocaine-d6 hydrochloride
    Inhibitor
    Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.
    Lidocaine-d<sub>6</sub> hydrochloride
  • HY-156671B
    RMC-4998 TFA
    Inhibitor 99.02%
    RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 TFA can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 TFA can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 TFA can be used for for non-small cell lung cancer (NSCLC) research.
    RMC-4998 TFA
  • HY-170916
    Angiogenesis inhibitor 7
    Inhibitor
    Angiogenesis inhibitor 7 (compound BT2) ia a potent inhibitor of angiogenesis. Angiogenesis inhibitor 7 inhibits ERK phosphorylation, FosB/ΔFosB and VCAM-1 expression.
    Angiogenesis inhibitor 7
  • HY-N7043R
    Isosilybin A (Standard)
    Inhibitor
    Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity[1][2][3].
    Isosilybin A (Standard)
  • HY-167237
    Calactin
    Activator
    Calactin is a glycoside that can be isolated from Asclepias curassavica L.. Calactin activates caspase-3, caspase-8, caspase-9, and phosphorylates ERK. Calactin induces DNA damage, apoptosis, PARP cleavage, G2/M phase cell cycle arrest, shifts Bax/Bcl-2 expression, and shows anti-proliferation effects in leukemia cells. Calactin can be used for the research of leukemia.
    Calactin
  • HY-101349A
    L 741742 hydrochloride
    Inhibitor
    L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma.
    L 741742 hydrochloride
  • HY-158969
    EGFR-IN-113
    Inhibitor
    EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.
    EGFR-IN-113
  • HY-15947G
    Ravoxertinib (GMP)
    Inhibitor
    Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma.
    Ravoxertinib (GMP)
  • HY-183284
    GZD-552
    Inhibitor
    GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme.
    GZD-552
  • HY-175271
    JWJ-01-378
    Inhibitor
    JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation.Pink: TRK ligand (HY-160520); Blue: CRBN ligase ligand (HY-103596); Black: linker
    JWJ-01-378
  • HY-168954
    CSF1R-IN-26
    Inhibitor
    CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22%.
    CSF1R-IN-26
  • HY-179119
    AB19
    Inhibitor
    AB19 is a potent Vav1 inhibitor. AB19 inhibits Vav1 and reduces its downstream ERK phosphorylation. AB19 shows anti-proliferative activity in pancreatic cancer models. AB19 can be used for pancreatic cancer research.
    AB19
  • HY-P11728
    Peptide E5
    Inhibitor
    Peptide E5 is an antagonist targeting the CXCR4/CXCL12 axis. Peptide E5 blocks the CXCR4/CXCL12 axis, downregulates CXCR4 expression, and inhibits the phosphorylation of downstream Akt and Erk. Peptide E5 induces apoptosis, suppresses migration and adhesion of breast cancer cells. Peptide E5 inhibits CXCL12-mediated endothelial progenitor cell recruitment, thereby suppressing tumor angiogenesis. Peptide E5 is applicable to relevant research on breast cancer.
    Peptide E5
  • HY-175257
    Theophylline-platinum(IV) prodrug-1
    Inhibitor
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
    Theophylline-platinum(IV) prodrug-1
  • HY-W040971R
    Creosol (Standard)
    Inhibitor
    Creosol (Standard) (2-Methoxy-4-methylphenol (Standard)) is the analytical standard of Creosol (HY-W040971). This product is intended for research and analytical applications. Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable.
    Creosol (Standard)
  • HY-148553
    Anti-inflammatory agent 36
    Inhibitor 98.01%
    Anti-inflammatory agent 36 is an anti-inflammatory agent. Anti-inflammatory agent 36 inhibits LPS-induced macrophage activation.
    Anti-inflammatory agent 36
  • HY-107622
    (E/Z)-BIX02188
    Inhibitor
    (E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
    (E/Z)-BIX02188
  • HY-180949
    EGFR-IN-189
    Inhibitor
    EGFR-IN-189 (Compound 7) is a selective covalent epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 200 nM. EGFR-IN-189 can effectively inhibit the C797S mutant type of EGFR. EGFR-IN-189 can inhibit cancer cells proliferation and inhibit EGFR phosphorylation and downstream ERK1/2 phosphorylation. EGFR-IN-189 can be used for research of nonsmall cell lung cancer.
    EGFR-IN-189
Cat. No. Product Name / Synonyms Application Reactivity

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