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-149414
    MY-673
    Inhibitor 98.60%
    MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro.
    MY-673
  • 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-16363
    Omtriptolide
    Omtriptolide (PG490-88) is a derivative proagent of triptolide purified from the Chinese herb.
    Omtriptolide
  • 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-P3206A
    Serum thymic factor acetate
    Inhibitor 99.80%
    Serum thymic factor acetate (Thymulin acetate) is the acetate salt form of Serum thymic factor (HY-P3206). Serum thymic factor acetate is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor acetate stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor acetate protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor acetate exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor acetate can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases.
    Serum thymic factor acetate
  • HY-142066
    4′-Demethylnobiletin
    Activator 99.78%
    4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling.
    4′-Demethylnobiletin
  • HY-N7110
    6-Hydroxyflavone
    Activator 99.95%
    6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role.
    6-Hydroxyflavone
  • 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-148552
    Anti-inflammatory agent 35
    Inhibitor 99.77%
    Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
    Anti-inflammatory agent 35
  • 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 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-19700S
    trans-Zeatin-d5
    Inhibitor 99.20%
    trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
    trans-Zeatin-d<sub>5</sub>
  • HY-N6076
    Tenuifoliside A
    Inhibitor 98.07%
    Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
    Tenuifoliside A
  • HY-P3751
    [Tyr8] Bradykinin
    Activator 99.61%
    [Tyr8] Bradykinin is a B2 kinin receptor agonist. [Tyr8] Bradykinin also stimulates ERK1/2 phosphorylation. [Tyr8] Bradykinin can be used as an internal standard.
    [Tyr8] Bradykinin
  • HY-114323
    PROTAC FLT-3 degrader 1
    Inhibitor 99.74%
    PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)).
    PROTAC FLT-3 degrader 1
  • HY-112082
    BAY885
    Inhibitor 99.27%
    BAY885 is a highly potent and selective ERK5 inhibitor with an IC50 of 35 nM. BAY885 shows weak inhibition on others kinases.
    BAY885
  • HY-111940
    LUT014
    Activator
    LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy.
    LUT014
  • HY-B0185B
    Lidocaine hydrochloride hydrate
    Inhibitor 99.90%
    Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate 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 hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine hydrochloride hydrate
  • HY-139192
    Brophenexin
    Activator 99.59%
    Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
    Brophenexin
  • HY-D0168
    Orcinol
    Activator 99.97%
    Orcinol (3,5-Dihydroxytoluene) is an organic compound used in biological dyeing and proteomics research. Orcinol inhibits melanogenesis in B16F10 cells by upregulating the MAPK/ERK signaling pathway, and suppresses the expression of MITF, tyrosinase (TYR), TRP1, and DCT. Orcinol exhibits certain DPPH radical scavenging activity. In addition, Orcinol can alter nitrogen balance in animals. Orcinol holds promise for research in cancer and metabolic diseases.
    Orcinol
Cat. No. Product Name / Synonyms Application Reactivity

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