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
All Product Categories
-
ERK Inhibitors
(733)
View all products
-
ERK Agonists
(10)
View all products
-
ERK Activators
(248)
View all products
-
ERK Modulators
(17)
View all products
-
ERK Chemical
(1)
View all products
-
ERK Inducers
(16)
View all products
-
ERK Degraders
(2)
View all products
-
ERK Controls
(3)
View all products
-
ERK Ligands
(2)
View all products
-
ERK Related Products (1114)
Related Products (1114)
-
Antibodies (22)
-
ERK Isoform Comparison
-
SBI-810 hydrochloride
0 ImagesSBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.
-
Mianserin
0 ImagesSynonyms: MianserineMianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
-
MT-125
0 ImagesCat. No.: HY-174406Purity: 98.73%MT-125 is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.
-
STX-721
0 ImagesSTX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations.
-
GPR34 receptor antagonist 3
0 ImagesGPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
-
Cornuside
0 ImagesCornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
-
Galloylpaeoniflorin
0 ImagesSynonyms: 6'-O-Galloyl paeoniflorinGalloylpaeoniflorin (6'-O-Galloyl paeoniflorin) is an orally active galloylated derivative of Paeoniflorin (HY-N0293) found in peony roots with various anti-inflammatory and antioxidant activities. Galloylpaeoniflorin suppresses RANKL-induced activation of ERK, JNK, c-Fos, c-Jun, and NFATc1, and reduces osteoclast-specific gene expression. Galloylpaeoniflorin activates Nrf2 and PI3K/Akt pathways, inhibits NF-κB activation, and scavenges ROS to reduce oxidative DNA, lipid, and protein damage. Galloylpaeoniflorin attenuates neuroinflammation, inhibits apoptosis, reduces Helicobacter pylori-induced gastric mucosa injury and UVB-induced cell damage. Galloylpaeoniflorin can be used for the research of osteoporosis, gastritis, ischemic stroke and skin diseases.
-
Notoginsenoside R2
0 ImagesSynonyms: 20(S)-Notoginsenoside R2; Ginsenoside Ng-R2Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside. Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ25-35-induced neuronal apoptosis and inflammatory responses. Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression. Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis.
-
Gallic aldehyde
0 ImagesGallic aldehyde (3,4,5-Trihydroxybenzaldehyde) is a phenolic aldehyde. Gallic aldehyde can be isolated from Geum japonicum. Gallic aldehyde inhibits the gelatinolytic activity and expression of MMP-9. Gallic aldehyde also inhibits ERK1/2, p38, and JNK. Gallic aldehyde has potent anti-HSV-1 and antioxidant activities. Gallic aldehyde also exhibits antibacterial activity against Oenococcus oeni VF.
-
R-IMPP
0 ImagesSynonyms: PF-00932239R-IMPP (PF-00932239) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.
-
Flavokawain A
0 ImagesFlavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
-
5-Methoxytryptophol
0 Images5-Methoxytryptophol is a 5-methoxyindole alcohol structurally homologous to Melatonin (HY-B0075). It is secreted by the mammalian pineal gland and exhibits an inverse circadian rhythm. 5-Methoxytryptophol regulates bone metabolism by activating the ERK1/2 pathway. It reduces the levels of pro-inflammatory cytokines TNF-α and IL-1β, as well as proteolytic enzymes MMP-1 and MMP-2, in serum and dental pulp tissues, thereby ameliorating acute pulpitis. 5-Methoxytryptophol induces rapid sleep in mice, while high doses cause respiratory depression and death. 5-Methoxytryptophol. 5-Methoxytryptophol can be used in studies related to acute pulpitis, hypnosis, and bone metabolism.
-
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside
![Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside](https://file.medchemexpress.com/product_pic/hy-n5084.gif "Click to View Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside Product Detail")
0 ImagesPinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8+ T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer.
-
GSK143 dihydrochloride
0 ImagesGSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
-
AT-533
0 ImagesAT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs).
