MEK

RO4927350 is a potent, selective MEK1/2 inhibitor, blocking MAPK pathway in vitro/vivo and showing notable antitumor effects.

Cobimetinib racemate (Cobimetinib (racemate)) (GDC-0973 racemate) is a selective inhibitor of MEK.Cobimetinib racemate is also known as a mitogen-activated

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.

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

Nedometinib (NFX-179) is a MEK1 inhibitor with anticancer and antitumor activities, which can be used to study malignant tumors.

GSK1790627, the N-deacetylated metabolite of Trametinib, represents an orally active MEK inhibitor that promotes autophagy and triggers apoptosis [1].

BAY-846: allosteric MEK inhibitor, long-lasting, highly bioavailable, low brain entry, effective in K-Ras A549 model.

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

MEK4 Inhibitor-2, a novel MEK4 inhibitor, demonstrates efficacy against pancreatic adenocarcinoma, exhibiting an IC50 value of 83 nM.

G-479, a potent MEK inhibitor and improved analogue of GDC-0623, has distributed polarity enhancing bioactivity.

Luvometinib is an inhibitor of the mitogen-activated protein kinase (MEK) with antitumor activity.

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

Atebimetinib, Oral MEK inhibitor, suppresses MAPK signaling, for combination therapy in metastatic pancreatic cancer and NSCLC.

MEK1/2-IN-2 is a potent, ATP-competitive MEK1/2 inhibitor that exhibits equal inhibitory effects on wild-type MEK1/2 and a group of MEK1/2 mutant cells.

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.