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-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-170982
    MS910
    		Inhibitor
    MS910 is an efficient and selective MEK1/2 PROTAC degrader. MS910 exhibits effective MEK1/2 degradation ability and anti proliferative activity in various cancer cells, such as HT-29 (MEK1 DC50 = 118 nM, MEK2 DC50 = 55 nM) and SK-MEL-28 (MEK1 DC50 = 94 nM, MEK2 DC50 = 38 nM) cells. MS910 is commonly used in cancer research. (Pink: MEK1/2 Ligand (HY-10254); Blue: CRBN Ligand (HY-W087383); Black: Linker (HY-W022240))
    MS910
  • 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-185446
    KZ-02
    		Inhibitor
    KZ-02 is an orally active dual MEK1/Pim-1 kinase inhibitor, with an IC50 of 1.07 nM against MEK1 and an IC50 of 1.34 μM against Pim-1. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.
    KZ-02
  • HY-174306
    MARY1
    		Inhibitor
    MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human 5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction.
    MARY1
  • 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-117404
    LLS30
    		Inhibitor
    LLS30 is an anticancer agent. LLS30 suppresses MEK/ERK pathway. LLS30 has anti-cancer effects against ovarian cancer, prostate cancer, and malignant peripheral nerve sheath tumors. LLS30 shows synergistic anti-cancer effect with Enzalutamide (HY-70002) or Docetaxel (HY-B0011).
    LLS30
  • HY-120339
    STK899704
    		Inhibitor
    STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ​​ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.
    STK899704
  • HY-N1988R
    Cucurbitacin IIa (Standard)
    		Inhibitor
    Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
    Cucurbitacin IIa (Standard)
  • 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-P5522
    TriDAP
    		Activator
    TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP decreases IκBα levels and increases p65 levels. TriDAP induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
    TriDAP
  • 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-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-183674
    MEK-IN-10
    		Inhibitor
    MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.
    MEK-IN-10
  • HY-E70844
    MAP2K2 Recombinant Human Active Protein Kinase
    MAP2K2 (MEK2) is a dual specificity protein kinase that belongs to the MAP kinase kinase family. This kinase is known to play a critical role in mitogen growth factor signal transduction. MAP2K2 phosphorylates and thus activates MAPK1/ERK2 and MAPK3/ERK1. MAP2K2 Recombinant Human Active Protein Kinase is a recombinant MAP2K2 protein that can be used to study MAP2K2-related functions.
    MAP2K2 Recombinant Human Active Protein Kinase
  • HY-112477A
    (E/Z)-Chk2-IN-1
    		Inhibitor
    (E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
    (E/Z)-Chk2-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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