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MEK

MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.

  • SCH772984
    T6066942183-80-4
    SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
    • $48
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  • MEK-IN-4
    T28012297744-42-4In house
    MEK-IN-4 is a MEK inhibitor that can be used to study inflammatory diseases and cancer.
    • $350 TargetMol
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  • Refametinib R enantiomer
    T12697923032-38-6In house
    Refametinib R enantiomer (RDEA119 R enantiomer) is an MEK inhibitor with an EC50 of 2.0-15 nM.Refametinib (R enantiomer) has anticancer activity and can be used in cancer research.
    • $85
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  • EF24
    T27242342808-40-6In house
    EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway.
    • $33
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  • PAF (C16)
    T2154774389-68-7In house
    PAF (C16) is a potent MAPK and MEK/ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.
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  • PD 198306
    T21980212631-61-3In house
    PD 198306 is a selective inhibitor of MAPK/ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.
    • $58
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  • Refametinib
    T6636923032-37-5In house
    Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).
    • $33
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  • Lidocaine hydrochloride
    T114473-78-9
    Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.
    • $45
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  • U0126-EtOH
    T62231173097-76-1
    U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
    • $30
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  • Honokiol
    T300135354-74-6
    Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
    • $50
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  • U0126
    T21332109511-58-2
    U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively. U0126 inhibits autophagy and mitophagy.
    • $110
    35 days
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    TargetMol | Citations Cited
  • Selumetinib
    T6218606143-52-6
    Selumetinib (AZD6244) (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).
    • $47
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  • PD98059
    T2623167869-21-8
    PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.
    • $34
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  • Mirdametinib
    T6189391210-10-9
    Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.
    • $47
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  • Trametinib
    T2125871700-17-3
    Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
    • $31
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  • Cobimetinib
    T3623934660-93-2
    Cobimetinib (GDC-0973) is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation.
    • $34
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  • Boehmenan
    TN352557296-22-7
    (±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell
    • $276
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  • Glycinexylidide
    T8063818865-38-8
    Glycinexylidide (GX), the active metabolite of the local anesthetic Lidocaine, exhibits properties significant in inhibiting sodium channels with complex voltage dependence and mitigates the proliferation and spread of gastric cancer cells. GX holds research promise in applications related to anesthesia, cancer, and cardiovascular disease [1].
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  • MS934
    T791432756323-15-4
    MS934, a novel VHL-recruiting MEK 1/2 degrader, exhibits potent anti-proliferative effects on HT-29 cell growth, achieving a GI50 of 0.023 μM. It holds potential for researching various human cancers including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma [1].
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  • Griffipavixanthone
    TN4166219649-95-3
    Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. It can inhibit tumor metastasis
    • $2,569
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  • Cajanin
    TN146232884-36-9
    Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it can significantly improve basal glucose uptake in HepG2 cells, its improving effect is concentration dependent, it exhibits effects stronger than that of rosiglitazone, which has been used as an antidiabetic drug.
    • $618
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  • Morusinol
    TN195362949-93-3
    Morusinol is a flavonoid extracted from the root bark of Morus alba. Morusinol has antiplatelet and anticancer activities, inhibits arterial thrombosis in vivo, and exerts antitumor activity by inducing autophagy, G2/M cell cycle blockade, inhibiting cell invasion and migration, and targeting the Ras/MEK/ERK pathway.
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    • Bufarenogin
      TN145917008-65-0
      Bufarenogin (3beta,12beta,14-Trihydroxy-11-oxo-5beta-bufa-20,22-dienolide) is a bufadienolide isolated from parotoid gland secretions of the Cuban endemic toad Peltophryne fustiger. Bufarenogin shows anti-tumor activity.
      • $72
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    • Ro 5126766
      T6971946128-88-7
      RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.
      • $52
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    • EBI-1051
      T151931801896-05-8
      EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).
      • $2,420
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    • BAY-6035
      T366312247890-13-5
      BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.
      • $48
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    • BMS-599626
      T2610714971-09-2
      BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
      • $558
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    • 5Z-7-Oxozeaenol
      T14055253863-19-3
      5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.
      • $215
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    • BIX02189
      T24161094614-85-3
      BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
      • $34
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    • GDC-0623
      T68431168091-68-6
      GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
      • $48
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    • BIX02188
      T1744334949-59-6
      BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.
      • $77
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    • Isorhamnetin
      T2836480-19-3
      Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LDL via inhibition of lectin-like ox-LDL receptor-1 upregulation, interference of ox-LDL-mediated intracellular signaling pathway (p38MAPK activation, NF-kappaB nuclear translocation, eNOS expression) and the antioxidant activity of isorhamnetin. Isorhamnetin prevents endothelial dysfunction, superoxide production, and overexpression of p47phox induced by angiotensin II. Isorhamnetin appears to be a potent drug against esophageal cancer due to it's in vitro potential to not only inhibit proliferation but also induce apoptosis of Eca-109 cells.
      • $34
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    • GW 284543 hydrochloride
      T7742179246-08-3
      GW 284543 hydrochloride is a selective inhibitor of MEK5 .
      • $51
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    • MEK inhibitor
      T11993334951-92-7
      MEK inhibitor is a potent MEK inhibitor with antitumor potency.
      • $219
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    • Epiberberine
      T5S23616873-09-2
      1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.
      • $31
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    • Corylifol C
      TN3711775351-91-2
      Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor receptor (EGFR): 1.1 and 4.4 × 10(-6) μg/ml, respectively).
      • $660
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    • Cobimetinib racemate
      T22677934662-91-6
      Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated protein kinase, is a key component of the RAS/RAF/MEK/ERK pathway.
      • $112
      5 days
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    • (E/Z)-BIX02188
      T63241094614-84-2
      BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.
      • $43
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    • Uncarinic acid E
      TN5201277751-61-8
      Uncarinic acid E has anti-cancer activity, it induces apoptosis in HepG2 cells via accumulation of p53, alters the Bax/Bcl-2 ratio, and activates caspases, resulting in cytochrome c release from the mitochondria. A mixture of uncarinic acid E and 27-O-p-(
      • $590
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    • anemarsaponin B
      T7030139051-27-7
      Anemarsaponin B has anti-inflammatory effect in LPS-treated RAW 264.7macrophages, the effect is associated with the inhibition of NF-κB transcriptional activity, possibly via the p38 MAP kinase pathway. Anemarsaponin B can inhibit PAF-induced rabbit platelet aggregation in vitro.
      • $84
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    • Binimetinib
      T2508606143-89-9
      Binimetinib (ARRY-162) (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.
      • $35
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    • SL327
      T2708305350-87-2
      SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.
      • $48
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    • ZM-447439
      T6077331771-20-1
      ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
      • $45
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    • trans-Zeatin
      TMS21811637-39-4
      trans-Zeatin ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.
      • $50
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    • GW284543
      T7610790186-68-4
      GW284543 (UNC10225170) is a selective inhibitor of MEK5 .
      • $31
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    • AZD8330
      T6083869357-68-6
      AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
      • $48
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    • Pimasertib
      T61311236699-92-5
      Pimasertib (AS703026) is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
      • $31
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    • PD318088
      T6152391210-00-7
      PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
      • $46
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    • MEK-IN-6 hydrate
      T790482845153-35-5
      MEK-IN-6 hydrate (compound 69), a MEK inhibitor, exhibits an IC50 value of 2 nM in A375 cells [1].
      • $1,670
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    • Nedometinib
      T782092252314-46-6
      Nedometinib, a tyrosine kinase inhibitor, specifically targets MEK1 and exhibits antineoplastic effects. It is utilized in research related to dermatosis, cutaneous fibroneruroma, and neurofibromatosis [1].
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