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-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-N0515R
    Ophiopogonin D (Standard)
    		Inhibitor
    Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D can be isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D can inhibit isteoclastic differentiation in RAW264.7 cells. Ophiopogonin D has protective effect as an antioxidant in H2O2-induced endothelial injury. Ophiopogonin D blocks ERK signaling cascades. Ophiopogonin D alleviates high-fat diet-induced metabolic syndrome and changes the structure of gut microbiota in mice. Ophiopogonin D has been used against inflammatory, metabolic and cardiovascular diseases.
    Ophiopogonin D (Standard)
  • 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-N7085R
    Citropten (Standard)
    		Inhibitor
    Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
    Citropten (Standard)
  • 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-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 SKOV3-BRCA1-KD 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-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-P10074
    TAT-MEK1
    		Inhibitor
    TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM.
    TAT-MEK1
  • HY-P5986
    mSIRK (L9A)
    		Control
    mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide.
    mSIRK (L9A)
  • HY-12736
    GSK143
    		Inhibitor
    GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
    GSK143
  • HY-167768
    SOS1 activator 2
    		Modulator
    SOS1 activator 2 (Compound 65) is a benzimidazole derivative and a SOS1 activator. SOS1 activator 2 has a high binding affinity for SOS1 with a Kd of 9 nM. SOS1 activator 2 can regulate the Ras-ERK signaling pathway, which can be used in the study of cancer.
    SOS1 activator 2
  • HY-112348
    HA-1004 hydrochloride
    		Inhibitor
    HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that 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 hydrochloride
  • HY-149759
    SHP2-IN-23
    		Inhibitor
    SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM.
    SHP2-IN-23
  • HY-P4497
    Prolylserine
    Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of ERK, but not cAMP response element binding protein (CREB).
    Prolylserine
  • HY-162888
    WQ-C-401
    		Inhibitor
    WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension.
    WQ-C-401
  • HY-N2510R
    Myristicin (Standard)
    		Inhibitor
    Myristicin (Standard) is the analytical standard of Myristicin. This product is intended for research and analytical applications. Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc.
    Myristicin (Standard)
  • HY-153350
    ERK-IN-7
    		Inhibitor
    ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent ERK inhibitor with IC50 of 5 nM and 7 nM against ERK1 and ERK2, respectively.
    ERK-IN-7
Cat. No. Product Name / Synonyms Application Reactivity
ERK Isoform Comparison

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