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MEK inhibitor

" in MedChemExpress (MCE) Product Catalog:

109

Inhibitors & Agonists

1

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2

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2

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4

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Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12202
    MEK inhibitor
    1 Publications Verification

    MEK Cancer
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
    <em>MEK</em> <em>inhibitor</em>
  • HY-15610
    GDC-0623
    5+ Cited Publications

    RG 7421; MEK inhibitor 1

    MEK Apoptosis Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
    GDC-0623
  • HY-139638

    MEK Cancer
    MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
    <em>MEK</em>4 <em>inhibitor</em>-1
  • HY-139639

    MEK Cancer
    MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
    <em>MEK</em>4 <em>inhibitor</em>-2
  • HY-157750

    MEK Raf Cancer
    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-P4133

    ERK MEK Cancer
    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 .
    <em>MEK</em>1 Derived Peptide <em>Inhibitor</em> 1
  • HY-P4136

    ERK Cancer
    Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM .
    Myristoyl-<em>MEK</em>1 Derived Peptide <em>Inhibitor</em> 1
  • HY-160414

    (R,R)-TRX-COBI; TRX-cobimetinib

    MEK Cancer
    TRX-COBI ((R,R)-TRX-COBI; Trx-cobimetinib) is a MEK inhibitor targeting TRX fragments based on Fe 2+. TRX-COBI has antitumor activity .
    TRX-COBI
  • HY-163173

    YAP Cancer
    TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
    TEAD-IN-8
  • HY-P5977

    Ste-MPKKKPTPIQLNP-NH₂; ERK Activation inhibitor Peptide

    ERK Cancer
    STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH?) is a cell permeable ERK1/2 inhibitor (IC50: 13-30?μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
    STE-MEK1(13)
  • HY-15496

    ER-806201

    MEK FLT3 Cancer
    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-15202
    Binimetinib
    20+ Cited Publications

    MEK162; ARRY-162; ARRY-438162

    MEK Autophagy Cancer
    Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib
  • HY-145701

    MEK Cancer
    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-14719
    RO4987655
    4 Publications Verification

    CH4987655

    MEK Cancer
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
    RO4987655
  • HY-12058
    AZD8330
    5+ Cited Publications

    ARRY-424704; ARRY-704

    MEK Cancer
    AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
    AZD8330
  • HY-137881

    MEK Inflammation/Immunology Cancer
    MEK-IN-4 is a MEK inhibitor. MEK-IN-4 can be used for the research of inflammatory disorders and cancers .
    MEK-IN-4
  • HY-153445A

    MEK Cancer
    MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC50 of 2 nM for A375 cells .
    MEK-IN-6 hydrate
  • HY-14691
    Refametinib
    10+ Cited Publications

    BAY 869766; RDEA119

    MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
    Refametinib
  • HY-U00312

    MEK Cancer
    MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.
    MEK-IN-1
  • HY-153445

    ERK MEK Cancer
    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-107622

    Others Metabolic Disease
    (E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
    (E/Z)-BIX02188
  • HY-50706
    Selumetinib
    55+ Cited Publications

    AZD6244; ARRY-142886

    MEK Apoptosis Cancer
    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-153864

    PROTACs MEK ERK Cancer
    PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
    PROTAC MEK1 Degrader-1
  • HY-15437
    SL327
    5+ Cited Publications

    MEK Cancer
    SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
    SL327
  • HY-143468

    Apoptosis MEK Cancer
    MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
    MEK-IN-5
  • HY-10999
    Trametinib
    150+ Cited Publications

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    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-145702

    MEK ERK Cancer
    MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
    MAP855
  • HY-13064A
    Cobimetinib hemifumarate
    30+ Cited Publications

    GDC-0973 hemifumarate; XL-518 hemifumarate

    MEK Apoptosis Cancer
    Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
    Cobimetinib hemifumarate
  • HY-18086
    TCS PIM-1 1
    3 Publications Verification

    SC 204330

    Pim Cancer
    TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
    TCS PIM-1 1
  • HY-50295
    CI-1040
    15+ Cited Publications

    PD 184352

    MEK Apoptosis Cancer
    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-13064
    Cobimetinib
    30+ Cited Publications

    GDC-0973; XL518

    MEK Apoptosis Cancer
    Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
    Cobimetinib
  • HY-10999S

    MEK Autophagy Apoptosis Cancer
    Trametinib-d4 is the deuterium 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[1][2].
    Trametinib-d4
  • HY-12055
    BIX02188
    3 Publications Verification

    MEK ERK Cancer
    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-12042
    Pimasertib
    5+ Cited Publications

    AS703026; MSC1936369B

    MEK Cancer
    Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
    Pimasertib
  • HY-10999A
    Trametinib (DMSO solvate)
    150+ Cited Publications

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    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-10999S1

    MEK Autophagy Apoptosis Cancer
    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[1][2].
    Trametinib-13C6
  • HY-10999S2

    GSK1120212-13C,d3; JTP-74057-13C,d3

    Isotope-Labeled Compounds MEK Autophagy Apoptosis Cancer
    Trametinib- 13C,d3 is the 13C- and deuterium 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[1][2].
    Trametinib-13C,d3
  • HY-50706A
    Selumetinib sulfate
    55+ Cited Publications

    AZD6244 sulfate; ARRY-142886 sulfate

    MEK Apoptosis Cancer
    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 sulfate
  • HY-18652
    Avutometinib
    1 Publications Verification

    Ro 5126766; CH5126766

    MEK Raf Cancer
    Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
    Avutometinib
  • HY-12031A
    U0126
    Maximum Cited Publications
    331 Publications Verification

    MEK Autophagy Mitophagy Influenza Virus Cancer
    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-107619

    MEK Cancer
    PD-334581 is a MEK1 inhibitor .
    PD-334581
  • HY-12062
    PD318088
    1 Publications Verification

    MEK Cancer
    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-107417

    VEGFR MEK FLT3 PDGFR ERK Cancer
    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/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
    Hypothemycin
  • HY-107621

    MEK Cancer
    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-P10074

    ERK Inflammation/Immunology
    TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM .
    TAT-MEK1
  • HY-12028
    PD98059
    280+ Cited Publications

    MEK ERK Aryl Hydrocarbon Receptor Autophagy Cancer
    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-126048

    MEK Cancer
    JTP-70902, a p15 INK4b-inductive compound, is a MEK1/2 inhibitor. JTP-70902 exhibits potent antitumor effect .
    JTP-70902
  • HY-131295
    PD0325901-O-C2-dioxolane
    2 Publications Verification

    MEK Ligands for Target Protein for PROTAC Cancer
    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-144692

    MEK PI3K PERK Cancer
    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-144693

    MEK PI3K PERK Cancer
    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

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