TAK-243

Description: TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis. Target: Apoptosis, E1/E2/E3 Enzyme, NF-kappaB. Smiles: NS(=O)(=O)OC[C@H]1C[C@@H](Nc2ccnc3cc(nn23)-c2cccc(SC(F)(F)F)c2)[C@H](O)[C@@H]1O. References: Zhuang J, et al. Ubiquitin-activating enzyme inhibition induces an unfolded protein response and overcomes drug resistance in myeloma. Blood. 2019 Apr 4,133(14):1572-1584.