molecules of the month

compound 41

oral WDR5 inhibitor

pM Ki, nanomolar in cells

from FBDD, SBDD, and PK opt.

J. Med. Chem.

Vanderbilt University School of Medicine, Nashville, TN

compound 41 chemical structure, oral WDR5 inhibitor - Vanderbilt University School of Medicine, Nashville, TN
4 mins read

Context.  “Compound 41” (Vanderbilt University School of Medicine) is an oral WD40 Repeat Domain 5 (WDR5) inhibitor being developed for various human cancers. The well-established role of epigenetic abnormalities in cancer development and progression has led to extensive studies to identify various epigenetic cancer inhibitors. Currently, seven such drugs have been approved by the FDA for diverse malignancies, and they target three major epigenetic drug targets: DNA methyltransferases (DNMTs), histone deacetylases (HDACs), and enhancer of zeste homolog 2 (EZH2). As a key mediator of multiple epigenetic regulatory complexes, WDR5 is emerging as an ideal epigenetic cancer target. Preclinical studies suggest that “compound 14” selectively targets cells with the mixed lineage leukemia (MLL) epigenetic signature through a potentially novel mechanism. In…

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