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

ERK

Extracellular signal regulated kinases

ERK

Related Products

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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.

ERK Isoform Specific Products:

ERK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-180794
    LHQ766
    		Inhibitor
    LHQ766 is a highly selective, orally active, covalent FGFR2 inhibitor with an IC50 of 7.3 nM. LHQ766 significantly suppresses phosphorylation of FGFR2 and its downstream signaling molecules FRS2-a, Akt and ERK1/2. LHQ766 selectively suppresses the proliferation of FGFR2-driven cancer cells.
    LHQ766
  • HY-180807
    MAPK-IN-6
    		Inhibitor
    MAPK-IN-6 (compound 116B) is a CNS-penetrant compound that inhibits the MAPK signaling pathway. MAPK-IN-6 reduces oxidative stress in SH-SY5Y neuronal cells by reducing ROS, restoring mitochondrial function, and inhibiting MAPK-driven inflammation. MAPK-IN-6 demonstrates profound neuroprotective efficacy in a rat tBCCAO/R model via ERK-P38-JNK signaling. MAPK-IN-6 can be used as a neuroprotective agent in ischemic stroke research.
    MAPK-IN-6
  • HY-180327
    NEPP11
    NEPP11 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.
    NEPP11
  • HY-50876A
    Daporinad hydrochloride
    		Inhibitor
    Daporinad (FK866) hydrochloride is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad hydrochloride depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad hydrochloride causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad hydrochloride induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad hydrochloride can be used for the study of myeloma, liver cancer, and immunosuppression.
    Daporinad hydrochloride
  • HY-N3807S
    Enniatin B1-13C34
    Enniatin B1-13C34 is the 13C-labeled Enniatin B1 (HY-N3807). Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
    Enniatin B1-<sup>13</sup>C<sub>34</sub>
  • HY-150587
    Anti-inflammatory agent 31
    		Inhibitor
    Anti-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.
    Anti-inflammatory agent 31
  • HY-118817
    Evariquinone
    		Inhibitor
    Evariquinone 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.).
    Evariquinone
  • HY-113756B
    rel-Latanoprost acid
    rel-Latanoprost acid is a relative configuration of Latanoprost acid (HY-113756A). Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
    rel-Latanoprost acid
  • HY-182749
    KRAS-IN-58
    		Inhibitor
    KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRASG12D. KRAS-IN-58 binds to KRASG12C and KRASG12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer.
    KRAS-IN-58
  • HY-P4159B
    Endothelin-1 (1-31) (Human) acetate
    		Activator
    Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) acetate is derived from the selective hydrolysis of big ET-1 by chymase.
    Endothelin-1 (1-31) (Human) acetate
  • HY-181800
    SHP2-IN-47
    		Inhibitor
    SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC50 of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2E76K (IC50 = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia.
    SHP2-IN-47
  • HY-130176
    UFP-512
    		Activator
    UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders.
    UFP-512
  • HY-W040971S
    Creosol-d4
    		Inhibitor
    Creosol-d4 (2-Methoxy-4-methylphenol-d4) is the deuterium labeled Creosol (HY-W040971). 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-d<sub>4</sub>
  • HY-182354
    VEGFR2-IN-84
    		Inhibitor
    VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors.
    VEGFR2-IN-84
  • HY-171581
    KRAS G12D-IN-27
    		Inhibitor
    KRAS G12D-IN-27 (H12a) is an inhibitor of KRAS G12D. KRAS G12D-IN-27 inhibits ERK phosphorylation, with an IC50 of 112 nM. KRAS G12D-IN-27 can be used in cancer research.
    KRAS G12D-IN-27
  • HY-181965
    KRAS G12C-IN-78
    KRAS 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.
    KRAS G12C-IN-78
  • HY-162460
    ERK1/2 inhibitor 10
    		Inhibitor
    ERK1/2 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.
    ERK1/2 inhibitor 10
  • HY-P5440
    ERKtide
    ERKtide is a biological active peptide. (ERKtide is a peptide substrate for ERK2. Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by mitogenic stimuli.)
    ERKtide
  • HY-W838814
    ERK1/2 inhibitor 12
    		Inhibitor
    ERK1/2 inhibitor 12 (compound 76.3) is a ERK1/2 inhibitor which inhibits ERK-mediated phosphorylation of caspase-9 and the p90Rsk-1 kinase. ERK1/2 inhibitor 12 exhibits anti-cancer activity and can be utilized in cancer research.
    ERK1/2 inhibitor 12
  • HY-P4136
    Myristoyl-MEK1 Derived Peptide Inhibitor 1
    		Inhibitor
    Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM.
    Myristoyl-MEK1 Derived Peptide Inhibitor 1
Cat. No. Product Name / Synonyms Application Reactivity
ERK Isoform Comparison

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