NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.
NUCC-0226272 (0.01-10 μM; 5 days) shows anti-proliferative effect in LNCaP and 22Rv1 cells[1]. NUCC-0226272 (10 μM; 6 days) shows strong degradation of EZH2, as well as reduction of PRC2 component SUZ12, and reduced H3K27me3 levels in C4-2B cells[1].
Pharmacokinetic Parameters of NUCC-0226272 in C57Bl/6 mouse[1].
References:
[1]. Gary E. Schiltz, et al. Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (ezh2) and proteolysis-targeting chimeric derivatives thereof (protacs) that induce degradation of ezh2. US20230346953A1.