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-RS08033
    MAP2K1 Human Pre-designed siRNA Set A
    		Inhibitor

    MAP2K1 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MAP2K1 Human Pre-designed siRNA Set A
    MAP2K1 Human Pre-designed siRNA Set A
  • HY-P4133
    MEK1 Derived Peptide Inhibitor 1
    MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable.
    MEK1 Derived Peptide Inhibitor 1
  • HY-162873
    MEK/RAF-IN-1
    		Inhibitor
    MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.
    MEK/RAF-IN-1
  • HY-139639
    MEK4 inhibitor-2
    		Inhibitor
    MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
    MEK4 inhibitor-2
  • HY-10999S1
    Trametinib-13C6
    		Inhibitor
    Trametinib-13C6 is the 13C-labeled Trametinib. 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-<sup>13</sup>C<sub>6</sub>
  • HY-144693
    MEK/PI3K-IN-2
    		Inhibitor
    MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.
    MEK/PI3K-IN-2
  • HY-157750
    MEK1/C-Raf-IN-1
    		Inhibitor
    MEK1/C-Raf-IN-1 (Compound 14d) is a MEK1/C-Raf inhibitor with IC50 values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity.
    MEK1/C-Raf-IN-1
  • HY-128634
    Anticancer agent 164
    		Inhibitor
    CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer.
    Anticancer agent 164
  • HY-N0103R
    Sophocarpine (Standard)
    		Inhibitor
    Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
    Sophocarpine (Standard)
  • HY-144692
    MEK/PI3K-IN-1
    		Inhibitor
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.
    MEK/PI3K-IN-1
  • HY-12042A
    Pimasertib hydrochloride
    		Inhibitor
    Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor.
    Pimasertib hydrochloride
  • HY-W357818
    Glycinexylidide
    		Inhibitor
    Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
    Glycinexylidide
  • HY-13303
    RO 4927350
    		Inhibitor
    RO 4927350 is a potent and selective non-ATP-competitive MEK1/2 inhibitor. RO 4927350 exhibits significant antitumor efficacy in a broad spectrum of tumor models.
    RO 4927350
  • HY-145701
    MEK1/2-IN-2
    		Inhibitor
    MEK1/2-IN-2 is a potent ATP-competitive MEK1/2 inhibitor and shows equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines.
    MEK1/2-IN-2
  • HY-N0776R
    Isorhamnetin (Standard)
    		Inhibitor
    Isorhamnetin (Standard) is the analytical standard of Isorhamnetin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-164400
    SIJ1777
    		Inhibitor
    SIJ1777 is a GNF-7 (HY-10943) derivative, possesses potent anti-cancer effects on melanoma cells harboring BRAF class I/II/III mutations. SIJ1777 substantially inhibits the activation of MEK, ERK, and AKT. SIJ1777 remarkably induces apoptosis and significantly blocks migration, invasion, and anchorage-independent growth of melanoma cells harboring BRAF class I/II/II mutations.
    SIJ1777
  • HY-13078S
    Cobimetinib-13C6 racemate
    		Inhibitor
    Cobimetinib-13C6 (GDC-0973-13C6; XL518-13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078). Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
    Cobimetinib-<sup>13</sup>C<sub>6</sub> racemate
  • HY-172803
    Ferroptosis inducer-7
    		Activator
    Ferroptosis inducer-7 is an orally active and selective ferroptosis inducer via inositol 1,4,5-trisphosphate receptor (IP3R)/calcium release-activated calcium channel protein (ORAI). Ferroptosis inducer-7 exhibits a notable effect in alleviating anemia symptoms, suppressing bone marrow CTLs activation, and improving hematopoietic function in immune-mediated bone marrow failure. Ferroptosis inducer-7 can be studied in research for aplastic anemia.
    Ferroptosis inducer-7
  • HY-RS08037
    Map2k2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Map2k2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k2 Mouse Pre-designed siRNA Set A
    Map2k2 Mouse Pre-designed siRNA Set A
  • HY-RS08036
    MAP2K2 Human Pre-designed siRNA Set A
    		Inhibitor

    MAP2K2 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MAP2K2 Human Pre-designed siRNA Set A
    MAP2K2 Human Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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