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MEK inhibitors act on mitogen-activated protein kinase kinases 1 and 2 (MEK1, MEK2) in growth factor signaling. MEK was cloned in 1992 as a protein kinase that phosphorylates the product of the extracellular signal-regulated kinase (ERK) gene. It is a dual-specificity enzyme that activates ERK1 and ERK2 by phosphorylating a threonine and a tyrosine residue. PD98059, reported in 1995, and U0126, reported in 1998 and listed as U0126-EtOH, were early synthetic MEK inhibitors. Trametinib, cobimetinib and binimetinib are allosteric MEK1/2 inhibitors used in studies of Ras- and Raf-driven signaling. (E/Z)-BIX 02189 instead targets MEK5, the kinase that activates ERK5. Inhibitors of the downstream kinases are listed in the sibling category ERK.
MS432 is a first-in-class, highly selective PROTAC degrader targeting MEK1 and MEK2, based on PD0325901 and a von Hippel-Lindau (VHL) E3 ligase ligand. It demonstrates favorable plasma exposure in mice and induces MEK1 and MEK2 degradation in HT29 cells with DC₅₀ values of 31 nM and 17 nM, respectively.
MS934 is a VHL-recruiting PROTAC degrader that targets MEK 1/2, facilitating their degradation alongside CRAF. This compound demonstrates significant biological activity in various cancer models, including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma. MS934 serves as an important tool for research into targeted cancer therapies and the mechanistic understanding of these oncogenic pathways.
PROTAC MEK1 Degrader-1 is a targeted protein degradation compound that selectively degrades MEK1 via a PROTAC mechanism. With a pIC50 value of 7.0, it effectively inhibits ERK1/2 phosphorylation, leading to downstream signaling modulation. This compound demonstrates significant antiproliferative activity against A375 melanoma cells, making it a valuable tool for research in cancer therapeutics and signaling pathway studies.
MS910 is a potent and selective PROTAC degrader targeting MEK1 and MEK2 kinases. It demonstrates effective degradation of MEK1 and MEK2 in various cancer cell lines, with reported DC50 values of 118 nM for MEK1 and 55 nM for MEK2 in HT-29 cells, and 94 nM for MEK1 and 38 nM for MEK2 in SK-MEL-28 cells. MS910 is primarily utilized in cancer research to explore the therapeutic potential of targeted protein degradation.
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