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-180419
    SF-3-030
    Inhibitor
    SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup.
    SF-3-030
  • HY-163709
    PROTAC FAK degrader 2
    Inhibitor
    PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer.
    PROTAC FAK degrader 2
  • HY-116091
    EGFR-IN-451
    Inhibitor
    EGFR-IN-451 is an EGFR inhibitor with an IC50 value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFRL858R, EGFRT790M, and EGFRL858R/T790M with IC50 values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer.
    EGFR-IN-451
  • HY-120406
    PLS-123
    Inhibitor
    LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.
    PLS-123
  • HY-59201
    A-582941
    Activator
    A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia.
    A-582941
  • HY-N7128R
    Flavanone (Standard)
    Inhibitor
    Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone (Standard)
  • HY-175803
    SHP2-IN-44
    Inhibitor
    SHP2-IN-44 (Compound 26) is an allosteric and orally active SHP2 inhibitor with an IC50 of 27 ?nM. SHP2-IN-44 also inhibits ERK phosphorylation (IC50 of 299 ?nM) without off-target hERG activity. SHP2-IN-44 has a broad-spectrum anticancer activity, such as juvenile myelomonocytic leukemia, neuroblastoma and breast cancer. SHP2-IN-44 can be used for Noonan syndrome, LEOPARD syndrome and cancers research.
    SHP2-IN-44
  • HY-181284
    BYBC-1
    Inhibitor
    BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (Kd = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer.
    BYBC-1
  • HY-RS08111
    Mapk15 Mouse Pre-designed siRNA Set A
    Inhibitor

    Mapk15 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mapk15 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Mapk15 Mouse Pre-designed siRNA Set A
  • HY-N18197
    Norkurarinol
    Inhibitor
    Norkurarinol is a prenylated flavonoid. Norkurarinol can be isolated from Sophora flavescens. Norkurarinol potently inhibits mushroom Tyrosinase DOPA oxidase activity with an IC50 of 2.1 μM. Norkurarinol inhibits poly(I:C)-induced NF-κB/AP-1 activation. Norkurarinol inhibits pro-inflammatory cytokines (TNF-α, IL-6). Norkurarinol inhibits phosphorylation of p38, JNK, and ERK1/2. Norkurarinol increases phosphorylation of IRF3. Norkurarinol has antiviral activity against Rotavirus KJ56-1
    Norkurarinol
  • HY-145027
    ERK1/2 inhibitor 5
    Inhibitor
    ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
    ERK1/2 inhibitor 5
  • HY-W142432S
    Perfluoroundecanoic acid-13C7
    Perfluoroundecanoic acid-13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.
    Perfluoroundecanoic acid-<sup>13</sup>C<sub>7</sub>
  • HY-B1272A
    Desipramine
    Activator
    Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
    Desipramine
  • HY-P3513A
    β-Neo-Endorphin acetate
    Activator
    β-Neo-Endorphin acetate is an endogenous opioid peptide. β-Neo-Endorphin acetate is a hypothalamic "big" Leu-enkephalin of porcine origin. β-Neo-Endorphin acetate shows activation of the Erk1/2, MMP-2 and MMP-9.
    β-Neo-Endorphin acetate
  • HY-169407
    AKT-IN-24
    Inhibitor
    KT-IN-24 (Compound M17) is a AKT allosteric inhibitor with anti-tumor activity. KT-IN-24 can target the AKT/mTOR and MEK/ERK signaling pathways and inhibit epithelial-mesenchymal transition, which has a synergistic suppressive effect on TNBC, promoting cell apoptosis while inhibiting proliferation and migration when used in combination with Trametinib (HY-10999).
    AKT-IN-24
  • HY-B1456AS
    Fenoprofen-13C6 sodium hydrate
    Activator
    Fenoprofen-13C6 (LILLY-53858-13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    Fenoprofen-<sup>13</sup>C<sub>6</sub> sodium hydrate
  • HY-173416
    Anti-inflammatory agent 100
    Inhibitor
    Anti-inflammatory agent 100 (Compound (+)-4S-23) is an anti-inflammatory agent. Anti-inflammatory agent 100 inhibits MAPK and NF-κB signaling, and also inhibits NF-κB pathway by suppressing the phosphorylation of IκB-α and blocking nuclear translocation of phosphorylated p65. Anti-inflammatory agent 100 inhibits NO production (IC50: 0.5 μM) and TNF-α, IL-6, IL-1β secretion.
    Anti-inflammatory agent 100
  • HY-175529
    KRASG12D-IN-7
    Inhibitor
    KRASG12D-IN-7 is a selective KRASG12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRASG12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRASG12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRASG12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC).
    KRASG12D-IN-7
  • HY-182004
    FLT3-IN-40
    Inhibitor
    FLT3-IN-40 is a type I ATP-competitive FLT3 inhibitor with an IC50 of 16.26 nM. FLT3-IN-40 reduces the autophosphorylation level of FLT3 and the phosphorylation level of downstream ERK. FLT3-IN-40 exhibits antiproliferative, cell cycle regulatory and apoptosis-inducing activities. FLT3-IN-40 can be used in research related to acute myeloid leukemia.
    FLT3-IN-40
  • HY-173483
    ATX inhibitor 26
    Inhibitor
    ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model.
    ATX inhibitor 26
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