MEK2
MEK2 (mitogen-activated protein kinase kinase 2) is a dual-specificity kinase that activates ERK1/2, regulating DNA repair, proliferation, and differentiation in mammalian cells[1][2]. Mechanistically, MEK2 interacts with the ribonucleotide reductase subunit p53R2, enhancing RNR activity under serum stimulation and after ionizing radiation, which supports nucleotide supply for DNA synthesis and repair[2]. Compared with MEK1, MEK2 can be sufficient for the proliferation of specific cancer cells, such as SK-MEL-28 melanoma cells, even when MEK1 activity is inhibited, indicating isoform-specific control of ERK-mediated proliferation[3]. In disease models, MEK2 knockdown selectively reduces invasive capacity in pancreatic cancer cells, highlighting its distinct contribution to tumor progression[4]. Inhibition of MEK2 also modulates TREM2 cell surface recruitment in microglia, linking MEK2 signaling to potential neuroinflammatory processes[5]. Pharmacological inhibitors targeting MEK2, either alone or in combination with MEK1 inhibitors, are being utilized in experimental applications for cancer and inflammatory models, demonstrating the utility of isoform-selective modulation[6][7][8]. Overall, MEK2 functions as a key regulator within the ERK/MAPK cascade, with specific roles in DNA repair, cellular proliferation, tumor invasiveness, and immune modulation, distinct from the overlapping but non-redundant activities of MEK1[4][2][3][7].
References:
- [1]. Werner U, et al. Die Vorbereitung hyperthyreoter Patienten auf die Operation [Preparation of hyperthyreotic patients for surgery]. Z Arztl Fortbild (Jena). 1975 May 15;69(10):531-5. German. [Content Brief]
- [2]. Mukherjee T, et al. Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment. Chemical Biology Letters. 2024;11(2):659.
- [3]. Schapansky J, et al. MEK1/2 activity modulates TREM2 cell surface recruitment. J Biol Chem. 2021 Jan-Jun;296:100218. [Content Brief]
- [4]. Bélanger LF, et al. Mek2 is dispensable for mouse growth and development. Mol Cell Biol. 2003 Jul;23(14):4778-87. [Content Brief]
- [5]. Piao C, et al. MEK2 regulates ribonucleotide reductase activity through functional interaction with ribonucleotide reductase small subunit p53R2. Cell Cycle. 2012 Sep 1;11(17):3237-49. [Content Brief]
- [6]. Lee CS, et al. MEK2 is sufficient but not necessary for proliferation and anchorage-independent growth of SK-MEL-28 melanoma cells. PLoS One. 2011 Feb 18;6(2):e17165. [Content Brief]
- [7]. Diamond EL, et al. Efficacy of MEK inhibition in patients with histiocytic neoplasms. Nature. 2019 Mar;567(7749):521-524. [Content Brief]
- [8]. Long ME, et al. MEK1/2 Inhibition Promotes Macrophage Reparative Properties. J Immunol. 2017 Jan 15;198(2):862-872. [Content Brief]
All Product Categories
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MEK2 Related Products (33)
Related Products (33)
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BI-847325
0 ImagesBI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Lixisenatide acetate
0 ImagesLixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
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Hypothemycin
0 ImagesCat. No.: HY-107417CAS No.: 76958-67-3
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DS03090629
0 ImagesCat. No.: HY-164474Purity: 99.16%DS03090629 is an orally active, ATP-competitive MEK1/2 inhibitor. DS03090629 binds to the ATP-binding pocket of MEK, and this binding is unaffected by phosphorylation status. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 nM and 0.15 nM, respectively. DS03090629 inhibits the MEK1F53L mutant while retaining activity relative to wild-type MEK1. DS03090629 suppresses the MAPK pathway, cell proliferation, and BRAF overexpression-mediated drug resistance in melanoma cells. DS03090629 can be used for research related to melanoma.
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(S)-N-trans-feruloyloctopamine
0 ImagesCat. No.: HY-N11517CAS No.: 640235-67-2(S)-N-trans-feruloyloctopamine is an isomer of N-trans-feruloyloctopamine (HY-N2232). N-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic husk, possessing tyrosinase inhibitory, FGF2 inhibitory, anti-melanogenic, and anti-tumor activities, and is used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.
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RO5068760
0 ImagesCat. No.: HY-111033CAS No.: 947182-25-4RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.
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MS910
0 ImagesCat. No.: HY-170982CAS No.: 2756323-28-9MS910 is a CRBN-recruiting MEK1/2 PROTAC degrader, with a DC50 of 94 nM against MEK1 and 38 nM against MEK2 in SK-MEL-28 cells. MS910 induces the degradation of GSPT1, IKZF1/3 and ZFP91, thereby inhibiting the downstream ERK signaling pathway and cancer cell growth. MS910 is applicable to research related to colorectal cancer and melanoma.
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GIT1-IN-1
0 ImagesCat. No.: HY-181978CAS No.: 844464-54-6GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.
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NEPP11
0 ImagesCat. No.: HY-180327CAS No.: 313051-12-6NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.
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Nuvrumetinib
0 ImagesCat. No.: HY-187882CAS No.: 3079099-31-0Synonyms: PAS-004Nuvrumetinib (PAS-004) is a macrocyclic MEK inhibitor. Nuvrumetinib functionally inhibits MEK1/2, thereby suppressing pERK in tumors. Nuvrumetinib inhibits the proliferation of NRAS-mutant cancer cells. Nuvrumetinib can be used in studies related to NRASG12C-mutant solid tumors, neurofibromatosis type 1 (NF1), RASopathies and laminopathies.
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CInQ-03
0 ImagesCat. No.: HY-130453CAS No.: 500272-80-0CInQ-03 is an allosteric inhibitor of MEK1/2, with IC50 values of 5 μM and 10 μM against MEK1 and MEK2, respectively. CInQ-03 inhibits the kinase activity of MEK1/2 and reduces the phosphorylation levels of downstream ERK1/2 and RSK. CInQ-03 suppresses both anchorage-dependent and anchorage-independent growth of colon cancer cells, the activity of AP-1 reporter gene in colon cancer cells, as well as EGF-induced growth, transformation and AP-1 reporter gene activity in HaCaT keratinocytes. CInQ-03 can be used in studies related to colon cancer.
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