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-10999
    Trametinib
    Inhibitor 99.96%
    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
  • HY-10254
    Mirdametinib
    Inhibitor 99.95%
    Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.
    Mirdametinib
  • HY-12028
    PD98059
    Inhibitor 99.96%
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
    PD98059
  • HY-12031A
    U0126
    Inhibitor 98.45%
    U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
    U0126
  • HY-50706
    Selumetinib
    Inhibitor 99.87%
    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
  • HY-402361
    TERT activator-1
    99.50%
    TERT activator-1 is a small molecule activator of telomerase reverse transcriptase (TERT). TERT activator-1 promotes TERT transcription through the MEK/ERK/AP-1 signaling cascade. TERT activator-1 promotes adult neurogenesis and enhances neuromuscular function. TERT activator-1 reduces cellular senescence and systemic inflammation in aged mice, and can be used in the study of aging.
    TERT activator-1
  • HY-172415
    Atebimetinib
    Inhibitor
    Atebimetinib is an inhibitor for MEK tyrosine kinase and exhibits antineoplastic activity.
    Atebimetinib
  • HY-169407
    AKT-IN-24
    Inhibitor
    KT-IN-24 (Compound M17) is a AKT allosteric inhibitor with anti-tumor activity. KT-IN-24 can target the AKT/mTOR and MEK/ERK signaling pathways and inhibit epithelial-mesenchymal transition, which has a synergistic suppressive effect on TNBC, promoting cell apoptosis while inhibiting proliferation and migration when used in combination with Trametinib (HY-10999).
    AKT-IN-24
  • HY-12031
    U0126-EtOH
    Inhibitor 99.41%
    U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
    U0126-EtOH
  • HY-13064
    Cobimetinib
    Inhibitor 99.81%
    Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
    Cobimetinib
  • HY-15202
    Binimetinib
    Inhibitor 99.28%
    Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib
  • HY-108635
    C16-PAF
    Activator 99.85%
    C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
    C16-PAF
  • HY-N0776
    Isorhamnetin
    Inhibitor 99.94%
    Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.
    Isorhamnetin
  • HY-18652
    Avutometinib
    Inhibitor 99.02%
    Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
    Avutometinib
  • HY-B0185
    Lidocaine
    Inhibitor 99.96%
    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.
    Lidocaine
  • HY-10999A
    Trametinib (DMSO solvate)
    Inhibitor 99.56%
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
    Trametinib (DMSO solvate)
  • HY-19700
    trans-Zeatin
    Inhibitor 99.83%
    trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
    trans-Zeatin
  • HY-158115
    NST-628
    Inhibitor 98.61%
    NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors.
    NST-628
  • HY-50295
    CI-1040
    Inhibitor 99.91%
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
    CI-1040
  • HY-12042
    Pimasertib
    Inhibitor 99.88%
    Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
    Pimasertib
Cat. No. Product Name / Synonyms Application Reactivity

MEK1

MEK2

MEK5

MEK

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

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%
Lixisenatide
MEK1
MEK2
  99.93%
GDC-0623
MEK1, Ki: 0.13 nM (+ATP)
   98.74%
Lidocaine hydrochloride   
MEK
99.84%
BIX02189  
MEK5, IC50: 1.5 nM
 99.99%
Trametiglue
MEK1
MEK2
  98.58%
Refametinib
MEK1, IC50: 19 nM
MEK2, IC50: 47 nM
  99.82%
APS-2-79
MEK1
   99.38%
TAK-733   
MEK, IC50: 3.2 nM
98.31%
Lidocaine (Standard)   
MEK
99.85%
AZD8330
MEK1, IC50: 7 nM
MEK2, IC50: 7 nM
  99.14%
SL327
MEK1, IC50: 180 nM
MEK2, IC50: 220 nM
  99.57%
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%
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
  99.21%
BIX02188  
MEK5, IC50: 4.3 nM
 99.85%
GW284543  
MEK5
 99.94%
Zapnometinib   
MEK, IC50: 5.7 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%
Nedometinib
MEK1, IC50: 135 nM
   98.25%
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