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-N5025
    Bullatine A
    		Inhibitor 98.0%
    Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression.
    Bullatine A
  • HY-12736A
    GSK143 dihydrochloride
    		Inhibitor 99.37%
    GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
    GSK143 dihydrochloride
  • HY-148877
    AT-533
    		Inhibitor 98.38%
    AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs).
    AT-533
  • HY-163828
    PPA24
    		98.09%
    PPA24 is a PP2A activator with a KD of 8.465 μM for PP2ACα. PPA24 induces cancer cell death via apoptosis. PP2ACα induces ROS generation and decreases the level of c-Myc expression. PPA24 can be used to study colorectal cancer (CRC), Folinic acid (HY-17556), 5-Fluorouracil (HY-90006), and Oxaliplatin (HY-17371) (FOLFOX)-resistant CRC, and melanoma cancer.
    PPA24
  • HY-N1504
    Loureirin B
    		Inhibitor 99.95%
    Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
    Loureirin B
  • HY-B0380A
    Trimebutine maleate
    		Inhibitor 99.91%
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate
  • HY-12833
    AMZ30
    		Inhibitor 99.76%
    AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma.
    AMZ30
  • HY-18285
    Longdaysin
    		Inhibitor 99.83%
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
    Longdaysin
  • HY-147405
    Tinlorafenib
    		Inhibitor 98.21%
    Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies.
    Tinlorafenib
  • HY-120006A
    (rel)-AR234960
    		Agonist 98.95%
    (rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure.
    (rel)-AR234960
  • HY-N2510
    Myristicin
    		Inhibitor 99.89%
    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
  • HY-N1941
    Isosinensetin
    		Inhibitor 99.90%
    Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc.
    Isosinensetin
  • HY-146195
    MAPK-IN-1
    		Inhibitor
    MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research.
    MAPK-IN-1
  • HY-14569
    CDPPB
    		Activator 98.01%
    CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease.
    CDPPB
  • HY-W001174
    2,5-Dihydroxyacetophenone
    		Inhibitor 99.89%
    2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
    2,5-Dihydroxyacetophenone
  • HY-P3418
    CKLF1-C27
    		Activator 98.46%
    CKLF1-C27, a C-terminal peptide of CKLF1, binds to CCR4 receptor and activates ERK1/2 pathway. CKLF1-C27 can abrogate the effect of CKLF1 on cells by competing for CCR4 receptor. CKLF1-C27 shows great effect on promoting proliferation on HUVECs. CKLF1-C27 has the potential for psoriasis research.
    CKLF1-C27
  • HY-134877
    BAY 2476568
    		Inhibitor 99.88%
    BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations.
    BAY 2476568
  • HY-B0185S1
    Lidocaine-d10
    		Inhibitor 99.58%
    Lidocaine-d10 is the deuterium labeled Lidocaine. 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-d<sub>10</sub>
  • HY-N1966
    (E)-Osmundacetone
    		Inhibitor 99.88%
    (E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress.
    (E)-Osmundacetone
  • HY-N2283
    Deltonin
    		Inhibitor 99.94%
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
    Deltonin
Cat. No. Product Name / Synonyms Application Reactivity
ERK Isoform Comparison

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