mek inhibitor

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.

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.

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.

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.

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.

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

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

iMDK quarterhydrate is a potent PI3K inhibitor that inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

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.

Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.

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

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

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.

NSC 80538 is an inhibitor of MEK Kinase PB1 Domains in multiplex HTS assays.

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

Cobimetinib R-enantiomer, the less active R-enantiomer of Cobimetinib, is a selective MEK inhibitor.

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

Balamapimod is a reversible inhibitor of Ras/Raf/MEK. It also has a potential anti-tumor activity.

DS03090629, an orally active MEK inhibitor, functions by competitively inhibiting MEK activity in the presence of ATP. This compound demonstrates strong binding affinity to both MEK and phosphorylated MEK, with dissociation constants (Kd) of 0.11 and 0.15 nM, respectively. It has shown efficacy in suppressing the proliferation of melanoma cell lines that overexpress BRAF mutations, achieving IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 is thus considered promising for anti-melanoma therapies.

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.

SJ-C1044 is an orally effective pan-RAF inhibitor demonstrating immunomodulatory and antitumor activities. It targets wild-type BRAF, wild-type CRAF, and BRAF(V600E) with IC50 values of 331, 257, and 187 nM, respectively. SJ-C1044 suppresses tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. Additionally, it shows inhibition of VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM respectively. The compound enhances the tumor immune microenvironment through inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is applicable for research in colorectal cancer.