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 Activators
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ERK Chemical
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ERK Inducers
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ERK Degraders
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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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TX2-121-1
0 ImagesCat. No.: HY-118998CAS No.: 1603845-42-6TX2-121-1 is a bifunctional hydrophobic tag Her3 degrader and also a Her3 inhibitor with an IC50 of 49 nM. TX2-121-1 covalently binds to Cys721 of Her3, induces Her3 degradation via the Hsp70/Hsp90-assisted proteasomal pathway, interferes with the heterodimerization of Her3 with Her2/c-Met, and attenuates downstream Erk/Akt signaling, thereby inhibiting Her3-dependent cancer cell growth. TX2-121-1 can be used for the research of non-small cell lung cancer, ovarian cancer and Her3-driven breast cancer.
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NMac1
0 ImagesCat. No.: HY-115507CAS No.: 1332290-68-2NMac1 is an orally active Nm23/NDPK activator. NMac1 directly binds to Nm23-H1 and activates the NDPK activity of recombinant Nm23-H1 with an EC50 of 10.7 uM. NMac1 induces AMPK activation and inhibits mTOR and ERK, leading to mitochondrial OXPHOS dysregulation and suppressing mitochondrial ROS production, which in turn induces mitochondrial dysfunction in MDA-MB-231 cells. NMac1 inhibits Complex I activity and suppresses changes in morphology and actin cytoskeleton organization following Rac1 activation in MDA-MB-231 cells. NMac1 inhibits tumor invasion, migration and metastasis. NMac1 is useful for studying metastatic tumors, such as breast cancer. NMac1 can be isolated from the ginger cassumunar Roxb.
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ERK2 IN-1
0 ImagesCat. No.: HY-112300CAS No.: 1093061-47-2
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Leupeptin
0 ImagesCat. No.: HY-18234CAS No.: 55123-66-5Leupeptin is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis.
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ERK-IN-2
0 ImagesCat. No.: HY-133084CAS No.: 2743576-56-7ERK-IN-2 is a ERK2 inhibitor with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.
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Revaprazan
0 ImagesCat. No.: HY-121851CAS No.: 199463-33-7Synonyms: SB 641257Revaprazan (SB 641257) is reversible proton pump inhibitor. Revaprazan can inhibit gastric acid secretion and protect gastric mucosa. Revaprazan can inhibit IkappaB-alpha degradation as well as Akt inactivation, resulting in attenuation of H. pylori-induced COX-2 expression. Revaprazan can be used for the researches of infection and inflammmation, such as H. pylori-infected gastric inflammation and gastric ulcer.
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ERK1/2 inhibitor 3
0 ImagesCat. No.: HY-145025CAS No.: 2737294-99-2ERK1/2 inhibitor 3 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 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1).
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Edaxeterkib
0 ImagesCat. No.: HY-139571CAS No.: 1695534-88-3
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Anti-inflammatory agent 99
0 ImagesCat. No.: HY-183934CAS No.: 1345412-48-7Anti-inflammatory agent 99 is a chalcone derivative. Anti-inflammatory agent 99 inhibits LPS (HY-D1056)-induced NF-κB nuclear translocation and suppress the phosphorylation of JNK, ERK, and p38. Anti-inflammatory agent 99 inhibits the expression of cytoinflammatory factors such as TNF-α and IL-6 induced by LPS. Anti-inflammatory agent 99 can be used for the research of LPS-induced septic shock.
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SNX-7081
0 ImagesCat. No.: HY-111165CAS No.: 908111-22-8SNX-7081 is an Hsp90 inhibitor with Ki and IC50 values of 26 nM and 44 nM, respectively. SNX-7081 blocks the nuclear translocation of NF-κB, inhibits the production of pro-inflammatory cytokines, attenuates the ERK/JNK and PDGF signaling pathways, and suppresses LPS (HY-D1056)-induced nitric oxide production. SNX-7081 inhibits DNA repair, induces G2/M cell cycle arrest, and triggers apoptosis via downregulation of MYC/nucleolin and activation of Fas. SNX-7081 can be used in research related to rheumatoid arthritis and cancer.
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Famotidine solution
0 ImagesCat. No.: HY-FLB0377CAS No.: 76824-35-6Synonyms: MK-208 solutionFamotidine solution is mainly composed of 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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Desipramine-d3
0 ImagesCat. No.: HY-B1272AS1CAS No.: 65100-49-4Desipramine-d3 is the deuterium labeled Desipramine (HY-B1272A). 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.
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Tauroursodeoxycholate-d5
0 ImagesCat. No.: HY-19696SCAS No.: 1207294-25-4Synonyms: Tauroursodeoxycholic acid-d5; TUDCA-d5; UR 906-d5Tauroursodeoxycholate-d5 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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Autotaxin-IN-8
0 ImagesCat. No.: HY-181931CAS No.: 3058084-21-9Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis.
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Isomaltulose monohydrate
0 ImagesCat. No.: HY-W745090CAS No.: 58024-13-8Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants.
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D-DT/MIF-1-IN-1
0 ImagesCat. No.: HY-181912CAS No.: 1461756-61-5D-DT/MIF-1-IN-1 (Compound 4h) is a non-competitive, non-covalent inhibitor of MIF-1 and D-DT, with IC50 values of 2.4 μM and 4.0 μM against D-DT, and an IC50 value of 9.8 μM against MIF-1. D-DT/MIF-1-IN-1 inhibits D-DT-induced phosphorylation of ERK and exerts antiproliferative activity in non-small cell lung cancer cells.
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BRSD-212
0 ImagesCat. No.: HY-189619BRSD-212 is an orally active KRAS G12V/G12D inhibitor. BRSD-212 binds the switch-II pocket and inhibits GDP- and GMPPNP-bound mutant KRAS, with IC50 <0.2 nM for both variants. BRSD-212 inhibits ERK phosphorylation in KRAS-mutant tumor cell lines. BRSD-212 induces tumor regression and inhibits tumor growth in xenograft models. BRSD-212 is well tolerated in murine tumor models with no body weight change. BRSD-212 can be used for the research of cancer.
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Anti-Big-ET-1 Antibody
0 ImagesCat. No.: HY-P991963
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UE01
0 ImagesCat. No.: HY-184501CAS No.: 486440-74-8UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer.
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Dehydrocrenatine
0 ImagesCat. No.: HY-N3711CAS No.: 26585-13-7
