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-12028
    PD98059
    Inhibitor 99.96%
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
    PD98059
  • HY-18723
    Yoda 1
    Activator 99.98%
    Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
    Yoda 1
  • HY-50846
    SCH772984
    Inhibitor 99.27%
    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
    SCH772984
  • HY-100489
    TBHQ
    Activator 99.88%
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
    TBHQ
  • HY-19696
    Tauroursodeoxycholate
    Inhibitor 99.91%
    Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
    Tauroursodeoxycholate
  • HY-121833
    Gambogic amide
    Activator
    Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke.
    Gambogic amide
  • HY-123468
    HA-1004
    Inhibitor 99.03%
    HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.
    HA-1004
  • HY-P10072A
    MK2-IN-5 acetate
    MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation.
    MK2-IN-5 acetate
  • HY-15816
    Ulixertinib
    Inhibitor 99.95%
    Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
    Ulixertinib
  • HY-N0003
    Honokiol
    Activator 99.90%
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
    Honokiol
  • HY-N0431
    Astragaloside IV
    Inhibitor ≥98.0%
    Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
    Astragaloside IV
  • HY-N2329
    Piperlongumine
    Inhibitor 99.87%
    Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.
    Piperlongumine
  • HY-19696A
    Tauroursodeoxycholate sodium
    Inhibitor 98.88%
    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
    Tauroursodeoxycholate sodium
  • HY-15947
    Ravoxertinib
    Inhibitor 99.75%
    Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
    Ravoxertinib
  • HY-101494
    Temuterkib
    Inhibitor 99.94%
    Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
    Temuterkib
  • HY-108635
    C16-PAF
    Activator 99.48%
    C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
    C16-PAF
  • HY-B0185
    Lidocaine
    Inhibitor 99.96%
    Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine 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 is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine
  • HY-12275
    FR 180204
    Inhibitor 99.64%
    FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively.
    FR 180204
  • HY-153346
    RMC-6291
    Inhibitor 99.65%
    RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM.
    RMC-6291
  • HY-12056
    BIX02189
    Inhibitor 99.99%
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
    BIX02189
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