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

MEK

MEK

Mitogen-activated protein kinase kinase; MAPKK; MAP2K

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10254G
    Mirdametinib (GMP)
    Inhibitor
    Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor.
    Mirdametinib (GMP)
  • HY-107621
    U0124
    ≥98.0%
    U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM.
    U0124
  • HY-153445
    MEK-IN-6
    Inhibitor 98.69%
    MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer.
    MEK-IN-6
  • HY-131295
    PD0325901-O-C2-dioxolane
    Inhibitor 98.62%
    PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
    PD0325901-O-C2-dioxolane
  • HY-107619
    PD-334581
    Inhibitor 99.72%
    PD-334581 is a MEK1 inhibitor.
    PD-334581
  • HY-107417
    Hypothemycin
    Inhibitor ≥98.0%
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/KDR/Flk-1/VEGFR1/Flt-1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
    Hypothemycin
  • HY-142042
    3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles
    Inhibitor 99.84%
    3-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.
    3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles
  • HY-B0185AS
    Lidocaine-d10 hydrochloride
    Inhibitor 99.79%
    Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. 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[2].
    Lidocaine-d<sub>10</sub> hydrochloride
  • HY-15496
    E6201
    Inhibitor
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy.
    E6201
  • HY-B0185S1
    Lidocaine-d10
    Inhibitor 98.89%
    Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. 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[2].
    Lidocaine-d<sub>10</sub>
  • HY-10216
    Refametinib (R enantiomer)
    Inhibitor
    Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
    Refametinib (R enantiomer)
  • HY-14947
    Balamapimod
    Inhibitor 99.47%
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
    Balamapimod
  • HY-N0811
    Anemarsaponin B
    Inhibitor
    Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
    Anemarsaponin B
  • HY-160414
    TRX-COBI
    Inhibitor
    TRX-COBI ((R,R)-TRX-COBI; Trx-cobimetinib) is a MEK inhibitor targeting TRX fragments based on Fe2+. TRX-COBI has antitumor activity.
    TRX-COBI
  • HY-139638
    MEK4 inhibitor-1
    Inhibitor 98.89%
    MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
    MEK4 inhibitor-1
  • HY-101522
    CHMFL-EGFR-202
    Inhibitor 99.75%
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ~10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
    CHMFL-EGFR-202
  • HY-B0185G
    Lidocaine (GMP)
    Inhibitor
    Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine 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.
    Lidocaine (GMP)
  • HY-10999R
    Trametinib (Standard)
    Inhibitor
    Trametinib (Standard) is the analytical standard of Trametinib. This product is intended for research and analytical applications. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
    Trametinib (Standard)
  • HY-N12740
    Napyradiomycin B4
    Inhibitor
    Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis.
    Napyradiomycin B4
  • HY-100627A
    APS-2-79 hydrochloride
    Antagonist
    APS-2-79 hydrochloride 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 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity

MEK1

MEK2

MEK5

MEK

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Please try each isoform separately.

MEK Inhibitors, Antagonists & Activators
Product NameMEK1MEK2MEK5MEKPurity    
Trametinib
MEK1, IC50: 2 nM
MEK2, IC50: 2 nM
  99.96%
Mirdametinib
MEK1, Ki: 1 nM
MEK2, Ki: 1 nM
 
MEK, IC50: 0.33 nM
99.95%
PD98059
MEK1, IC50: 2-7 μM
MEK2, IC50: 50 μM
  99.96%
U0126
MEK1, IC50: 70 nM
MEK2, IC50: 60 nM
  98.45%
Selumetinib
MEK1, IC50: 14 nM
  
MEK, IC50: 12 nM
99.87%
TERT activator-1
MEK1
MEK2
  99.50%
U0126-EtOH
MEK1, IC50: 70 nM
MEK2, IC50: 60 nM
  99.41%
Cobimetinib
MEK1, IC50: 4.2 nM
   99.81%
Binimetinib   
MEK, IC50: 12 nM
99.28%
C16-PAF   
MEK
99.85%
Isorhamnetin
MEK1
   99.94%
Avutometinib   
MEK, IC50: 160 nM
99.02%
Lidocaine   
MEK
99.96%
Trametinib (DMSO solvate)
MEK1, IC50: 2 nM
MEK2, IC50: 2 nM
  99.56%
trans-Zeatin   
MEK
99.83%
CI-1040
MEK1, IC50: 17 nM
   99.91%
Pimasertib
MEK1
MEK2
  99.88%
GDC-0623
MEK1, Ki: 0.13 nM (+ATP)
   98.74%
Lixisenatide
MEK1
MEK2
  99.93%
BIX02189  
MEK5, IC50: 1.5 nM
 99.99%
Lidocaine hydrochloride   
MEK
99.96%
Trametiglue
MEK1
MEK2
  98.58%
Refametinib
MEK1, IC50: 19 nM
MEK2, IC50: 47 nM
  99.82%
TAK-733   
MEK, IC50: 3.2 nM
98.31%
AZD8330
MEK1, IC50: 7 nM
MEK2, IC50: 7 nM
  99.14%
APS-2-79
MEK1
   99.38%
MS432
MEK1, DC50: 31 nM (in HT29 cells)
MEK1, DC50: 31 nM (in SK-MEL-28 cells)
MEK2, DC50: 17 nM (in HT29 cells)
MEK2, DC50: 9.3 nM (in SK-MEL-28 cells)
  99.78%
Lidocaine (Standard)   
MEK
99.85%
SL327
MEK1, IC50: 180 nM
MEK2, IC50: 220 nM
  99.57%
RGB-286638
MEK1, IC50: 54 nM
   99.70%
Azelnidipine
MEK1
MEK2
  99.66%
MAP855
MEK1, IC50: 3 nM
   98.48%
BI-847325 
MEK2, IC50: 4 nM
  98.15%
Tunlametinib
MEK1
MEK2
  98.25%
RO4987655
MEK1, IC50: 5.2 nM
MEK2, IC50: 5.2 nM
  99.26%
GW284543  
MEK5
 99.94%
Zapnometinib   
MEK, IC50: 5.7 nM
99.85%
BIX02188  
MEK5, IC50: 4.3 nM
 99.85%
PD318088
MEK1
MEK2
  99.91%
Cobimetinib hemifumarate
MEK1, IC50: 4.2 nM
   99.73%
RGB-286638 free base
MEK1, IC50: 54 nM
   98.07%
PD 198306   
MEK
99.75%
MEK inhibitor   
MEK
98.35%
PD184161   
MEK, IC50: 10-100 nM
98.08%
Lidocaine hydrochloride hydrate   
MEK
99.90%
MEK-IN-6   
MEK
98.69%
PD0325901-O-C2-dioxolane
MEK1
MEK2
  98.62%
PD-334581
MEK1
   99.72%
Hypothemycin
MEK1, Ki: 17 nM
MEK2, Ki: 38 nM
  ≥98.0%
E6201
MEK1, IC50: 5.2 nM
   
Refametinib (R enantiomer)   
MEK, EC50: 2-15 nM
Balamapimod   
MEK
99.47%
CHMFL-EGFR-202
MEK1, IC50: 161 nM
   99.75%
APS-2-79 hydrochloride
MEK1
   
GW284543 hydrochloride  
MEK5
 
MEK/RAF-IN-1
MEK1, IC50: 28 nM
   
MEK/PI3K-IN-2
MEK1, IC50: 352 ± 2 nM
   
MEK/PI3K-IN-1
MEK1, IC50: 124 ± 11 nM
   
Isorhamnetin (Standard)
MEK1
   
MEK1-IN-1
MEK1, : 10.29 nM
   
MEK-IN-6 hydrate   
MEK
MEK-IN-1   
MEK