MEK
Mitogen-activated protein kinase kinase (MEK), primarily represented by MEK1 (MAP2K1) and MEK2 (MAP2K2), is a dual-specificity protein kinase that phosphorylates and activates extracellular signal-regulated kinases ERK1 and ERK2, thereby functioning as a central signaling relay within the MAPK/ERK cascade[1][2]. MEK operates downstream of RAS and RAF kinases and transduces extracellular and intracellular signals into programs controlling cell proliferation, differentiation, survival, transcriptional regulation, and development[2][3][4]. Mechanistically, RAF-mediated activation of MEK enables phosphorylation of ERK proteins at the conserved Thr-Glu-Tyr motif, leading to signal propagation through the canonical MAPK pathway[2][5]. Aberrant activation of MEK signaling has been associated with multiple human diseases, including melanoma, lung cancer, ovarian cancer, leukemia, lymphoma, and developmental disorders linked to dysregulated RAS/MAPK signaling[2][6][7]. Compared with other MAP2K family members that regulate the p38 or JNK pathways, MEK1 and MEK2 function specifically within the ERK signaling branch, providing pathway selectivity and making them key experimental targets for dissecting MAPK-dependent biological responses[1]. For experimental applications, pharmacological MEK inhibitors including trametinib, selumetinib, cobimetinib, binimetinib, mirdametinib, and avutometinib are widely used to suppress ERK activation and investigate MEK-dependent signaling mechanisms in cancer and developmental biology models[2].
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MEK Related Products (149)
Related Products (149)
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Antibodies (2)
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Lidocaine-d10
0 ImagesLidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine 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 is an amide derivative and has potential for the research of ventricular arrhythmia.
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Zapnometinib
0 ImagesSynonyms: PD0184264; ATR-002Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.
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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.
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Broussoflavonol F
0 ImagesCat. No.: HY-N9330CAS No.: 162558-94-3Broussoflavonol F is a potent dual inhibitor of the HER2-RAS-MEK-ERK signaling pathway and mushroom tyrosinase with an IC50 value of 82.3 μM. Broussoflavonol F downregulates the expression of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk proteins. Broussoflavonol F induces cell cycle arrest and apoptosis, and exhibits cytotoxicity in colon cancer cells. Broussoflavonol F inhibits endothelial proliferation, migration and tube formation, suppresses subintestinal vascular development, and reduces the mRNA levels of angiogenesis-associated genes.Broussoflavonol F can be used for colon cancer research.
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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.
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Cobimetinib racemate
0 ImagesSynonyms: GDC-0973 racemate; XL518 racemateCobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
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Luvometinib
0 ImagesSynonyms: FCN-159Luvometinib is a mitogen-activated protein kinase (MEK) inhibitor with antitumor activity.
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DZ2002
0 ImagesDZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.
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Polfurmetinib
0 ImagesSynonyms: MEK-IN-6
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3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles
0 Images3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM. 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is inhibitor for mitogen-activated protein kinase 1 (MEK1). 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles exhibits anti-inflammatory and neuroprotective activity in EAE mouse model.
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Lidocaine-d10 hydrochloride
0 ImagesLidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride 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, an amide derivative, has the potential for the research of the ventricular arrhythmia.
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Cobimetinib (R-enantiomer)
0 ImagesSynonyms: GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
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Simetryn
0 ImagesSimetryn is a triazine herbicide that exerts teratogenicity. Simetryn inhibits photosynthesis by blocking electron transfer in the chloroplast photosystem II and activates the MEK/Erk signaling pathway. Simetryn triggers vascular and developmental abnormalities in zebrafish and tadpoles, suppresses proliferation, enhances apoptosis, and induces malformations. Simetryn serves as a tool to establish a zebrafish model for studying arteriovenous malformations and related pathogenesis. Simetryn controls paddy weeds and can be used for research on developmental and vascular disorders.
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MEK inhibitor
0 ImagesMEK inhibitor is a potent MEK inhibitor with antitumor potency.
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Glycinexylidide
0 ImagesCat. No.: HY-W357818CAS No.: 18865-38-8Synonyms: GXGlycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
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GSK1790627
0 ImagesGSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis.
