MEK Inhibitor

DZ2002 (Standard) is the analytical standard of DZ2002. This product is intended for research and analytical applications. DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

Refametinib (Standard) is the analytical standard of Refametinib. This product is intended for research and analytical applications. Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.

PD 198306 (Standard) is the analytical standard of PD 198306 (HY-107620). This product is intended for research and analytical applications. PD 198306 is a selective MAPK/ERK-K_inase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.

Cobimetinib (racemate) (Standard) is the analytical standard of Cobimetinib (racemate). This product is intended for research and analytical applications. Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

G-479 is the inhibitor for MEK and hERG channel (IC₅₀=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC₅₀ of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats.

Binimetinib (Standard) is the analytical standard of Binimetinib. This product is intended for research and analytical applications. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.

U0126-EtOH (Standard) is the analytical standard of U0126-EtOH (HY-12031). This product is intended for research and analytical applications. U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

Luvometinib-d (FCN-159-d) is the deuterated-labeled Luvometinib (HY-159846). Luvometinib is an orally potent MEK1/2 inhibitor. Luvometinib selectively blocks the MAPK signaling pathway by forming a ternary complex with MEKase and ATP, thereby reducing the phosphorylation level of ERK. Luvometinib induces cell cycle arrest and apoptosis, and inhibits cancer cell proliferation. Luvometinib can be used in relevant research on various solid tumors including melanoma, non-small cell lung cancer, colon cancer, and acute myeloid leukemia.

MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.