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-178955
    EGFR-IN-182
    Inhibitor
    EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer.
    EGFR-IN-182
  • HY-N0213R
    Peiminine (Standard)
    Peiminine (Standard) is the analytical standard of Peiminine. This product is intended for research and analytical applications. Peiminine is a compound that can be isolated from Bolbostemma paniculatum (Maxim) Franquet (Cucurbitaceae family). Peiminine can induce apoptosis in human hepatocellular carcinoma HepG2 cells through both extrinsic and intrinsic apoptotic pathways. Peiminine has anti-inflammatory, anticancer, anti-osteoporosis, cardioprotective and other activities in many animal models.
    Peiminine (Standard)
  • HY-N3806S
    Enniatin B-13C33
    Enniatin B-13C33 is the 13C-labeled Enniatin B (HY-N3806). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).
    Enniatin B-<sup>13</sup>C<sub>33</sub>
  • HY-111000
    BNC-1
    BNC-1 is an Elk-1 activator that can promote phosphorylation and activation of Elk-1.
    BNC-1
  • HY-B1092AS2
    Gluconate-d6 sodium
    Gluconate-d6 sodium (D-Gluconic acid sodium salt-d6) is the deuterium labeled Gluconate sodium (HY-B1092A). Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
    Gluconate-d<sub>6</sub> sodium
  • HY-150187
    20:4 Lyso PI
    Activator
    20:4 Lyso PI acts as an activator of GPR55 and RhoA. 20:4 Lyso PI activates the GPR55-RhoA-ROCK pathway, thereby inducing morphological changes, cytoskeleton assembly, cell rounding and stress fiber formation. 20:4 Lyso PI can be used in research related to diseases such as those of the nervous system.
    20:4 Lyso PI
  • HY-179732
    PROTAC ALK degrader-4
    Inhibitor
    PROTAC ALK degrader-4 (Compound B8) is an ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 exhibits excellent anti-proliferative activity against NCI-H2228 and NCI-H3122. PROTAC ALK degrader-4 leads to a significant downregulation of 390 proteins, including IGF-1R and its downstream proteins such as ERK1/2 and STAT3. PROTAC ALK degrader-4 can be used for research on lung adenocarcinoma. (Pink: ALK ligand (HY-15656); Blue: CRBN ligand (HY-179733); Black: linker).
    PROTAC ALK degrader-4
  • HY-172221
    SOS1-IN-18
    Inhibitor
    SOS1-IN-18 (Compound 8) is the inhibitor for Son of Sevenless 1 protein (SOS1) with a KD of 2.6 nM, and inhibits SOS1-KRAS G12C interaction with an IC50 of 3.4 nM. SOS1-IN-18 inhibits the phosphorylation of ERK in H358 with an IC50 of 31 nM, inhibits the proliferation of H358 with an IC50 of 5 nM.
    SOS1-IN-18
  • HY-161363
    ERK2 allosteric-IN-1
    Inhibitor
    ERK2 allosteric-IN-1 (compound 1) is a selective and allosteric ERK2 inhibitor with the IC50 of 11 μM.
    ERK2 allosteric-IN-1
  • HY-N0747R
    Oxypeucedanin (Standard)
    Inhibitor
    Oxypeucedanin (Standard) is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin (Standard) is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin (Standard) induces cell cycle arrest and apoptosis. Oxypeucedanin (Standard) inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin (Standard) exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
    Oxypeucedanin (Standard)
  • HY-176733
    HDAC6-IN-61
    HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC50: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a GPR40 activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease.
    HDAC6-IN-61
  • HY-181232
    Anticancer agent 301
    Inhibitor
    Anticancer agent 301 is an anticancer agent. Anticancer agent 301 selectively downregulates the phosphorylation level of ERK1/2 without affecting the NF-κB p65 subunit. Anticancer agent 301 exhibits antiproliferative activity against breast cancer cells and can be used in breast cancer-related research.
    Anticancer agent 301
  • HY-149717
    Antitumor agent-122
    Antitumor agent-122 is a potent multi-target antitumor agent that exerts its effects through the induction of ferroptosis, autophagy, apoptosis, and cell cycle arrest. In the ferroptosis pathway, Antitumor agent-122 inhibits GPX4 expression and upregulates FACL4 expression, increasing intracellular lipid peroxidation and ferrous ion levels. In the autophagy pathway, Antitumor agent-122 induces autophagy by inhibiting the AKT/mTOR signaling pathway. In the apoptosis and cell cycle pathways, Antitumor agent-122 arrests cells at the G1/S phase and subsequently promots mitochondrial pathway-mediated apoptosis. Antitumor agent-122 can be used in the research of solid tumors including gastric, liver, ovarian, and bladder cancers.
    Antitumor agent-122
  • HY-117356A
    MRS2693 ammonium
    Activator
    MRS2693 ammonium is the ammonium dalt form of MRS2693 (HY-117356). MRS2693 ammonium is a selective agonist for P2Y6 with an EC50 of 0.015 μM. MRS2693 ammonium protects C2C12 skeletal muscle cells from TNFα-induced apoptosis. MRS2693 ammonium reduces the activation of NF-kB, activates the ERK1/2 pathway, and has a cytoprotective effect on mouse ischemia-reperfusion injury model[2].
    MRS2693 ammonium
  • HY-181670
    WH23
    Inhibitor
    WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.
    WH23
  • HY-115907
    K20
    Inhibitor
    K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity.
    K20
  • HY-138135
    OP-1118
    Inhibitor
    OP-1118 (Fidaxomicin metabolite OP-1118) is an orally active dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739).
    OP-1118
  • HY-172916
    LC-SF-14
    Inhibitor
    LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC50 values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research.
    LC-SF-14
  • HY-181587
    PDGFRA/CAIX/XII-IN-1
    Inhibitor
    PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.
    PDGFRA/CAIX/XII-IN-1
  • HY-156394
    Laxiflorin B-4
    Inhibitor
    Laxiflorin B-4 is modificative compound of Laxiflorin B (HY-156393), exhibited higher affinity for ERK1/2 and stronger tumor suppression.
    Laxiflorin B-4
Cat. No. Product Name / Synonyms Application Reactivity

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