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-Y0271R
    Urea (Standard)
    		Activator
    Urea (Standard) is the analytical standard of Urea. This product is intended for research and analytical applications. Urea is a powerful protein denaturant via both direct and indirect mechanisms. A potent emollient and keratolytic agent. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
    Urea (Standard)
  • HY-114491A
    Rineterkib hydrochloride
    		Inhibitor 99.81%
    Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.
    Rineterkib hydrochloride
  • HY-N2082
    Isorhamnetin 3-O-galactoside
    		Inhibitor 99.64%
    Isorhamnetin 3-O-galactoside (Cacticin) is a flavonoid glycoside that can be isolated from Oenanthe javanica, with antithrombotic and profibrinolytic activities. Isorhamnetin 3-O-galactoside inhibits the activities of thrombin and factor Xa (FXa) and reduces thrombin-catalyzed fibrin polymerization maximum rate. Isorhamnetin 3-O-galactoside suppresses TNF-α-induced PAI-1 secretion, decreases the PAI-1/tissue-type plasminogen activator (t-PA) ratio, and inhibits FXa production and FVa/FXa-mediated thrombin generation. Isorhamnetin 3-O-galactoside exerts protective effects against Carbon tetrachloride (CCl4) (HY-Y0298)-induced hepatic injury in mice. Isorhamnetin 3-O-galactoside can be used for the study of liver injury-related diseases and thrombotic vascular diseases.
    Isorhamnetin 3-O-galactoside
  • HY-14928A
    Lobeglitazone sulfate
    		Inhibitor 99.63%
    Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.
    Lobeglitazone sulfate
  • HY-N7043
    Isosilybin A
    		Inhibitor 99.63%
    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
  • HY-129636
    CLH304a
    		Inhibitor
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor.
    CLH304a
  • HY-123468
    HA-1004
    		Inhibitor 99.04%
    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 is 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
  • 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-N8303
    Gardenin A
    		Activator
    Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects.
    Gardenin A
  • HY-128393
    Trilinolein
    		Inhibitor ≥98.0%
    Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.
    Trilinolein
  • HY-W040971
    Creosol
    		Inhibitor 99.82%
    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
  • HY-19696AS
    Tauroursodeoxycholate-d4 sodium
    		Inhibitor 99.50%
    Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. 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-d<sub>4</sub> sodium
  • HY-101481
    Flurbiprofen axetil
    		Inhibitor 99.34%
    Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.
    Flurbiprofen axetil
  • 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-N4090
    Vicenin 3
    		Inhibitor 99.90%
    Vicenin 3 is an angiotensin-converting enzyme (ACE) inhibitor (IC50 = 46.91 μM) that can be isolated from the aerial parts of Desmodium styracifolium. Vicenin 3 ameliorates IL-1β-induced extracellular matrix degradation in SW1353 chondrocytes by regulating the MAPK pathway. Vicenin 3 can be used for the study of osteoarthritis (OA) and hypertension.
    Vicenin 3
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
ERK Isoform Comparison

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