MLN7243

MLN7243 is a cell permeable small molecule inhibitor targeting ubiquitin-activating enzymes (UAE, also known as E1 enzymes). The enzymes, found more active in cancer cells than in normal, healthy cells, catalyze the first step in ubiquitination reaction, targeting a protein for degradation via Proteasome. This covalent attachment of ubiquitin or ubiquitin-like proteins to targeted proteins is a major mechanism for regulating protein function in eukaryotic organisms. Inhibition of the enzyme prevents both protein ubiquitination and subsequent ubiquitin-mediated proteasomal degradation, resulting in an excess of proteins in the cells that may lead to endoplasmic reticulum (ER) stress-mediated apoptosis, thus inhibit tumor (cancer) cell proliferation and survival. MLN7243 is the first-in-class inhibitor specifically targeting this class of enzyme to be studied clinically.

Soluble in DMSO