mek

MEK-IN-4 is a MEK inhibitor utilized in the study of inflammatory diseases and cancer.

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.

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.

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.

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.

Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).

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

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.

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

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).

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.

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

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

MEK RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

MEK inhibitor is a tyrosine kinase receptor and cell cycle protein CDK complex inhibitor with antitumor activity and can be used to study tumor cell proliferation.

MEK-IN-1 is a MEK inhibitor that serves as a chemical compound used in biological research to inhibit the activity of MEK enzymes.

MEK ligand-2, a ligand for the target protein for PROTAC (Ligand for Target Protein for PROTAC), functions as an inhibitor for both MEK1 and MEK2. This compound plays a crucial role in MS934, which is a VHL-recruiting MEK1 2 PROTAC degrader.

Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1 2 (IC50: 2 nM).

MEK PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), effectively reducing pAKT and pERK1 2 levels and exhibiting anti-proliferative activity against various tumor cell lines [1].

MEK-IN-6 (Example 69), a potent MEK inhibitor, effectively inhibits ERK1 2 (Thr202 Tyr204) phosphorylation in A375 cells, with an IC50 of 2 nM, making it valuable for cancer research [1].

MEK-IN-5, a potent MEK inhibitor and nitric oxide (NO) donor, effectively decreases pMEK and pERK levels in a dose-dependent and time-dependent fashion. Additionally, it induces apoptosis in MDA-MB-231 cells.

MEK PI3K-IN-1 (compound 6r) is a potent dual inhibitor of MEK and PI3K, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. It effectively reduces pAKT and pERK1 2 levels, demonstrating anti-proliferative effects on various tumor cell lines [1].

MEK1 2-IN-3 (Compound M15) is an inhibitor of MEK1, with an IC50 value of 10.29 nM. It effectively suppresses tumor cell proliferation and migration, induces apoptosis, and exhibits good liver microsomal stability. MEK1 2-IN-3 is applicable in the study of solid tumors.

MEK4 inhibitor-1 is a newly developed compound specifically designed to inhibit the activity of MEK4, a key enzyme involved in pancreatic adenocarcinoma, with an IC 50 value of 61 nM.