2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. MEK

MEK

Mitogen-activated protein kinase kinase; MAPKK; MAP2K

MEK

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MEK (Mitogen-activated protein kinase kinase, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinases (MAPKs). The activated MAPK leads to the phosphorylation of downstream transcription factors that regulate various responses such as stress signaling, pathogen response, and hormone signaling.

In general, the MAPKKK phosphorylates a serine or threonine residue on a MAPKK, which sequentially activates a MAPK (ERK, p38 or JNK), the last protein in the cascade. Activation of the p38 MAPK occurs mainly through mitogen-activated protein kinase kinase 3 (MKK3) and MKK6 (sometimes MKK4). The JNK is regulated by two upstream MAP2Ks: MKK4 and MKK7. The highly homologous kinases, MEK1 and MEK2, act downstream of Ras and Raf to activate ERK mitogen-activated protein kinases.

MEK Isoform Specific Products:

MEK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15610
    GDC-0623
    		Inhibitor 99.15%
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
    GDC-0623
  • HY-13449
    TAK-733
    		Inhibitor 98.31%
    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
    TAK-733
  • HY-B0185A
    Lidocaine hydrochloride
    		Inhibitor 99.96%
    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 is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.
    Lidocaine hydrochloride
  • HY-50706A
    Selumetinib sulfate
    		Inhibitor 99.59%
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
    Selumetinib sulfate
  • HY-14691
    Refametinib
    		Inhibitor 99.82%
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
    Refametinib
  • HY-130602
    MS432
    		Inhibitor 99.78%
    MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
    MS432
  • HY-18955
    BI-847325
    		Inhibitor 98.66%
    BI-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.
    BI-847325
  • HY-100627
    APS-2-79
    		Antagonist 99.48%
    APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling.
    APS-2-79
  • HY-12058
    AZD8330
    		Inhibitor 99.14%
    AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
    AZD8330
  • HY-153181
    Trametiglue
    		Inhibitor 98.58%
    Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions.
    Trametiglue
  • HY-15504
    RGB-286638
    		Inhibitor 99.84%
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638
  • HY-15437
    SL327
    		Inhibitor ≥98.0%
    SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
    SL327
  • HY-P0119
    Lixisenatide
    		99.93%
    Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe−/− Irs2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation.
    Lixisenatide
  • HY-14719
    RO4987655
    		Inhibitor 99.26%
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
    RO4987655
  • HY-114189
    GW284543
    		Inhibitor 99.99%
    GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
    GW284543
  • HY-145702
    MAP855
    		Inhibitor 99.38%
    MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.
    MAP855
  • HY-12055
    BIX02188
    		Inhibitor 99.85%
    BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
    BIX02188
  • HY-12062
    PD318088
    		Inhibitor 99.91%
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research.
    PD318088
  • HY-139558
    Zapnometinib
    		Inhibitor 99.63%
    Zapnometinib (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.
    Zapnometinib
  • HY-119917
    Gossypetin
    		Inhibitor 99.82%
    Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
    Gossypetin
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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