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.
ERK Isoform Specific Products
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ERK Inhibitors
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ERK Agonists
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ERK Activators
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ERK Modulators
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ERK Chemical
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ERK Inducers
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ERK Degraders
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ERK Controls
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ERK Ligands
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ERK Related Products (1167)
Related Products (1167)
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Antibodies (22)
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ERK Isoform Comparison
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Propoxur (Standard)
0 ImagesPropoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
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Trimebutine-d3 hydrochloride
0 ImagesCat. No.: HY-B0380S2Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride 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 hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
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SHP1-IN-2
0 ImagesCat. No.: HY-186140SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research.
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Antitumor agent-226
0 ImagesCat. No.: HY-189265CAS No.: 3056235-77-6Antitumor agent-226 is a DNMT3A inhibitor and epigenetic modulator. Antitumor agent-226 inhibits cell proliferation and migration by downregulating DNA Methyltransferase, reducing global DNA methylation, and modulating JNK, ERK1/2, and p38 phosphorylation through the MAPK pathway to induce mitochondria-dependent apoptosis, G2/M phase arrest, autophagy, and ROS production. Antitumor agent-226 can be used for research on prostate cancer.
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SHP2/NAMPT-IN-1
0 ImagesCat. No.: HY-184650SHP2/NAMPT-IN-1 is an orally active dual inhibitor of SHP2 and NAMPT, with IC50 values of 30.5 nM and 24.4 nM, respectively. SHP2/NAMPT-IN-1 reduces NAD+ levels and p-ERK expression by inhibiting NAMPT. SHP2/NAMPT-IN-1 can inhibit the migration and colony formation of MDA-MB-231 cells and promote apoptosis. SHP2/NAMPT-IN-1 has anti-proliferative activity against a variety of tumor cell lines and can reverse PD-L1-mediated T-cell immunosuppression. SHP2/NAMPT-IN-1 can be used for breast cancer research.
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Lidocaine hydrochloride hydrate (Standard)
0 ImagesSynonyms: Lignocaine hydrochloride hydrate (Standard)Lidocaine (hydrochloride hydrate) (Standard) is the analytical standard of Lidocaine (hydrochloride hydrate). This product is intended for research and analytical applications. 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.
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C11 peptide-1
0 ImagesCat. No.: HY-P11827C11 peptide-1 is an antifibrotic agent that binds directly to Collagen I. C11 peptide-1 physically disrupts Collagen I interaction with Lumican. C11 peptide-1 reduces inflammatory infiltration and inhibits the ERK1/2 and Smad2/3 signaling pathways. C11 peptide-1 can be used for the research of liver fibrosis.
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Emodic acid
0 ImagesEmodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells.
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MK2-IN-5
0 ImagesCat. No.: HY-P10072CAS No.: 474713-20-7Synonyms: Hsp25 kinase inhibitor; Mk2 pseudosubstrateMK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation.
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Avicin G
0 ImagesCat. No.: HY-134505CAS No.: 197787-17-0Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer.
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Cudraflavone B
0 ImagesCat. No.: HY-N10009CAS No.: 19275-49-1Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells.
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GSK-3β/VEGFR2-IN-1
0 ImagesCat. No.: HY-184741GSK-3β/VEGFR2-IN-1 is an orally active dual inhibitor of GSK-3β (IC50 = 325 nM) and VEGFR2 (IC50 = 78 nM). GSK-3β/VEGFR2-IN-1 suppresses the phosphorylation of VEGFR2, AKT, MEK and ERK, inhibits human tongue squamous cell carcinoma cells migration and suppresses formation of HUVECs, exhibits low toxicity towards other cancer cells and normal cells, demonstrates significant antitumor efficacy in a CAL27 xenograft mouse model. GSK-3β/VEGFR2-IN-1 can be used for the study of tongue squamous cell carcinoma.
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Sitagliptin hydrochloride
0 ImagesCat. No.: HY-13749ECAS No.: 486459-71-6Synonyms: MK-0431 hydrochlorideSitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
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EUK-189
0 ImagesCat. No.: HY-19382CAS No.: 186350-27-6EUK-189 is a synthetic superoxide dismutase (SOD) and catalase mimetic. EUK-189 can block oxygen/glucose deprivation (OGD)-induced ERK1/2 dephosphorylation, ATP depletion and eliminate ROS production. EUK-189 exhibits neuroprotective effect and can inhibit delayed radiation injury. EUK-189 can be used for the research of neurological disease, such as ischemic stroke.
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Dinitramine
0 ImagesCat. No.: HY-W714183CAS No.: 29091-05-2Dinitramine is a herbicide. Dinitramine activates the Erk/P38/JNK/MAPK pathway and inactivates the PI3k/Akt pathway in testicular cells. Dinitramine induces endoplasmic reticulum stress, dysregulation of calcium homeostasis in the cytoplasm and mitochondria, apoptosis, and downregulated expression of cell cycle genes in testicular cells. Dinitramine reduces the viability and proliferation capacity of testicular cells, and inhibits cell division by suppressing the synthesis of tubulin. Dinitramine induces abnormal heart development, inhibited angiogenesis, inflammatory responses, apoptosis, and impaired embryonic growth in zebrafish embryos.
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ERK5-IN-4
0 ImagesCat. No.: HY-150606CAS No.: 1888305-17-6
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EGFR-IN-218
0 ImagesCat. No.: HY-189291CAS No.: 2410789-80-7EGFR-IN-218 is an orally effective EGFR inhibitor with IC50 values of 3.85, 0.40, and 140.5 nM against EGFRWT, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. EGFR-IN-218 inhibits EGFR phosphorylation and downstream ERK1/2 signaling, and exhibits in vivo antitumor activity. EGFR-IN-218 can be used for research on EGFR-mutant non-small cell lung cancer, glioblastoma, and brain metastasis.
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Famotidine-13C,d3
0 ImagesCat. No.: HY-B0377SCAS No.: 2744683-81-4Synonyms: MK-208-13C,d3Famotidine-13C,d3 (MK-208-13C,d3) is the deuterated, 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.
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Gestodene (Standard)
0 ImagesCat. No.: HY-B0110RCAS No.: 60282-87-3Synonyms: SHB 331 (Standard); WL 70 (Standard)Gestodene (Standard) (SHB 331 (Standard); WL 70 (Standard)) is the analytical standard of Gestodene (HY-B0110). This product is intended for research and analytical applications. Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.
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Akt/NF-κB/MAPK-IN-1
0 ImagesCat. No.: HY-149496CAS No.: 2994215-72-2Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent and orally active inhibitor against NO (IC50=7.70 μM) with no significant toxicity. Akt/NF-κB/MAPK-IN-1 shows anti-inflammatory activity by inhibiting Akt/NF-κB and MAPK signaling pathways.
