MEK

SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.

MEK-IN-4 is a MEK inhibitor that can be used to study inflammatory diseases and cancer.

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.

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.

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.

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.

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).

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.

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.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.

U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).

Selumetinib (AZD6244) (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).

AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

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.

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.

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.

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.

(±)-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

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].

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].

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

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.

EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

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.

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.

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.

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.

GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

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.

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.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

GW 284543 hydrochloride is a selective inhibitor of MEK5 .

MEK inhibitor is a potent MEK inhibitor with antitumor potency.

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.

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).

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.

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.

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-(

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.

Binimetinib (ARRY-162) (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.

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.

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.

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.

trans-Zeatin ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing.

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.

Pimasertib (AS703026) is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.

GW284543 (UNC10225170) is a selective inhibitor of MEK5 .

MEK-IN-6 hydrate (compound 69), a MEK inhibitor, exhibits an IC50 value of 2 nM in A375 cells [1].

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].