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-162888
    WQ-C-401
    Inhibitor 99.41%
    WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension.
    WQ-C-401
  • HY-164853
    Kanglexin
    99.65%
    Kanglexin is an orally active and novel anthraquinone compound. Kanglexin inhibits NLRP3 inflammatory body activation and cell pyroptosis, and has a cardioprotective effect. Kanglexin promotes angiogenesis through FGFR1/ERK signaling pathway and accelerates diabetic wound healing. In addition, Kanglexin has the effect of lipid-lowering and inhibiting the dedifferentiation of vascular smooth muscle cells, and can be used in the study of hyperlipidemia, fatty liver and atherosclerosis.
    Kanglexin
  • HY-176528
    PROTAC ERK5 degrader-1
    Inhibitor 99.58%
    PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity, such as acute lymphoblastic leukemia.
    PROTAC ERK5 degrader-1
  • HY-126858
    Ambuic acid
    Inhibitor 98.00%
    Ambuic acid exhibits antimicrobial activity against Staphylococcus aureus, with IC50 of 43.9 μM for strain ATCC 6538. Ambuic acid is an inhbitor for the biosynthesis of cyclic peptide quorum sensing molecules (quormones) in gram-positive bacteria. Ambuic acid exhibits anti-inflammatory activity through ERK/JNK/MAPK signaling pathway.
    Ambuic acid
  • HY-156671A
    RMC-4998 formic
    Inhibitor 99.02%
    RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research.
    RMC-4998 formic
  • HY-158990
    GE1111
    Inhibitor
    GE1111 is a MRGPRX2 antagonist (IC50 = 9.4 μM). GE1111 inhibits MRGPRX2/MRGPRB2-mediated mast cell activation. GE1111 reduces the expressions of TSLP, IL-13, MCP-1, TNF-α, IL-1β and periostin, maintains the expression levels of claudin 1 and involucrin, restores the phagocytic activity of macrophages, and attenuates the activation of STIM1 and phosphorylated AKT. GE1111 exerts anti-inflammatory and anti-allergic effects in multiple animal models. GE1111 is applicable to the research related to rosacea, atopic dermatitis and ulcerative colitis.
    GE1111
  • HY-149616
    PPM-3
    Degrader 98.2%
    PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages.
    PPM-3
  • HY-116269
    AZA197
    Inhibitor 98.71%
    AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts. AZA197 can be used for the study of colon cancer.
    AZA197
  • HY-142026
    Vitisin A
    Inhibitor
    Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
    Vitisin A
  • 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-123647
    Satratoxin H
    Activator 99.7%
    Satratoxin H is a toxic metabolite of Stachybotrys atra. Satratoxin H induces caspase-3 and PARP cleavage via p38 MAPK and JNK pathways, stimulates JNK, ERK, and p38 MAPK phosphorylation, and activates JNK and p38 MAPK in a glutathione-sensitive manner. Satratoxin H induces DNA double-stranded breaks, apoptotic body formation, intracellular reactive oxygen species generation, and endoplasmic reticulum stress via ATF6, PERK, and IRE1 pathways. Satratoxin H can be used for the research of central nervous system disorders and melanoma.
    Satratoxin H
  • HY-121280
    ERK2-IN-4
    Inhibitor 99.9%
    ERK2-IN-4 (Compound 6o) is an effective and selective ERK2 inhibitor with a Ki of 0.006 μM. ERK2-IN-4 inhibits the ERK signaling pathway and can be used in cancer research.
    ERK2-IN-4
  • HY-P10728
    B7-33
    Activator 99.31%
    B7-33 is a single-chain relaxin mimetic and a selective relaxin receptor 1 (RXFP1) agonist. B7-33 phosphorylates ERK1/2 without inducing activation of the cAMP signaling pathway. B7-33 exhibits anti-fibrotic and cardioprotective activities. B7-33 can be used in the research of vascular diseases such as cardiomyopathy, myocardial infarction and fibrosis.
    B7-33
  • HY-165298
    DGY-09-192
    Inhibitor 99.50%
    DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)).
    DGY-09-192
  • HY-N4042
    Hirsutenone
    Inhibitor 99.74%
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
    Hirsutenone
  • HY-156450
    ERK5-IN-5
    Inhibitor 99.05%
    ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells.
    ERK5-IN-5
  • HY-122664
    XMU-MP-2
    Modulator 99.29%
    XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC50 of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research.
    XMU-MP-2
  • HY-168669
    PROTAC K-Ras Degrader-5
    Inhibitor
    PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer.
    PROTAC K-Ras Degrader-5
  • HY-N1910
    4'-O-Methylbavachalcone
    99.64%
    4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy.
    4'-O-Methylbavachalcone
  • 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
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