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-N6576
    Hellebrigenin
    Inhibitor 99.69%
    Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers.
    Hellebrigenin
  • HY-N2736
    3′,4′,7-Trihydroxyflavone
    Inhibitor 98.0%
    3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC50 = 1.89 μM) and COX-1 (IC50 = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H2O2-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice.
    3′,4′,7-Trihydroxyflavone
  • HY-113599
    Isoprocurcumenol
    Activator
    Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes.
    Isoprocurcumenol
  • HY-152293
    EVT801
    Inhibitor
    EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models. EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EVT801
  • HY-13463A
    Avatrombopag maleate
    Activator 99.88%
    Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
    Avatrombopag maleate
  • HY-161275
    BI-4732
    Inhibitor 99.30%
    BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC).
    BI-4732
  • 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-B0444R
    Maprotiline hydrochloride (Standard)
    Maprotiline (hydrochloride) (Standard) is the analytical standard of Maprotiline (hydrochloride). Maprotiline (hydrochloride) (Standard) is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline (hydrochloride) (Standard) induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.
    Maprotiline hydrochloride (Standard)
  • HY-B1556S
    Benzyl salicylate-d4
    Inhibitor 99.01%
    Benzyl salicylate-d4 (NSC 6647-d4) is the deuterium labeled Benzyl salicylate (HY-B1556). Benzyl salicylate (NSC 6647)?is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber.
    Benzyl salicylate-d<sub>4</sub>
  • HY-W744699
    Larixol
    Inhibitor
    Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants.
    Larixol
  • HY-139192A
    Brophenexin free base
    Activator 99.24%
    Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
    Brophenexin free base
  • HY-124404A
    12(S)-HETE
    Inducer 99.10%
    12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells.
    12(S)-HETE
  • HY-137440A
    Firazorexton hydrate
    Inducer 99.94%
    Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice.
    Firazorexton hydrate
  • HY-100489R
    TBHQ (Standard)
    Activator
    TBHQ (Standard) is the analytical standard of TBHQ. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N4042
    Hirsutenone
    Inhibitor 99.74%
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
    Hirsutenone
  • HY-D0885D
    Phosphocreatine disodium hydrate
    Activator 99.57%
    Phosphocreatine (disodium hydrate) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine (disodium hydrate) enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine (disodium hydrate) normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine (disodium hydrate) Phosphocreatine (disodium hydrate) provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway..
    Phosphocreatine disodium hydrate
  • HY-117291A
    XMD-17-51 TFA
    99.46%
    XMD-17-51 TFA is a pyrimido-diazepinone compound that is able to modulate protein kinases.
    XMD-17-51 TFA
  • HY-N7085
    Citropten
    Inhibitor 99.41%
    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
  • HY-153738
    ERK1/2 inhibitor 9
    Inhibitor
    ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2.
    ERK1/2 inhibitor 9
  • HY-122246
    ML192
    Inhibitor
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
    ML192
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