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-132844
    Tunlametinib
    		Inhibitor 98.25%
    Tunlametinib, an antineoplastic agent, is a MEK1/2 inhibitor.
    Tunlametinib
  • HY-114189
    GW284543
    		Inhibitor 99.99%
    GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
    GW284543
  • HY-139558
    Zapnometinib
    		Inhibitor 99.85%
    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-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-13064A
    Cobimetinib hemifumarate
    		Inhibitor 99.73%
    Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
    Cobimetinib hemifumarate
  • 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-148907
    CS640
    		Inhibitor 99.43%
    CS640 is a selective inhibitor of calmodulin-dependent kinases. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4 and MLK3 with IC50 values of 0.08, 0.03, 0.001, 0.001, 11.2, 0.025, 5.69 and 2.75 μM, respectively. CS640 also shows inhibitory effects to CYP450 2C9 and CYP450 2C19 with IC50 values of 6 and 10 μM, respectively.
    CS640
  • HY-13078
    Cobimetinib racemate
    		Inhibitor 99.71%
    Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
    Cobimetinib racemate
  • HY-15504A
    RGB-286638 free base
    		Inhibitor 98.07%
    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 free base
  • HY-16446
    SAR125844
    		98.17%
    SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.
    SAR125844
  • HY-156625
    Nedometinib
    		Inhibitor 98.25%
    Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. Nedometinib has antineoplastic effect and can be used for research in dermatosis, cutaneous fibroneuroma, neurofibromatosis.
    Nedometinib
  • HY-12202
    MEK inhibitor
    		Inhibitor 98.35%
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
    MEK inhibitor
  • HY-148507
    GSK1790627
    		Inhibitor 98.81%
    GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis.
    GSK1790627
  • HY-19700S
    trans-Zeatin-d5
    		Inhibitor 99.2%
    trans-Zeatin-d5 is deuterium labeled trans-Zeatin. 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-d<sub>5</sub>
  • HY-10174
    PD184161
    		Inhibitor 98.08%
    PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior.
    PD184161
  • HY-13079
    Cobimetinib (R-enantiomer)
    		Inhibitor 99.78%
    Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
    Cobimetinib (R-enantiomer)
  • HY-B0185B
    Lidocaine hydrochloride hydrate
    		Inhibitor 99.90%
    Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate 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 hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine hydrochloride hydrate
  • 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-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-107620
    PD 198306
    		Inhibitor 99.75%
    PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.
    PD 198306
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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