UBCS039

UBCS039 is a synthetic small molecule that acts as a first-in-class activator of Sirtuin 6 (SIRT6), an NAD+-dependent histone deacetylase. By specifically enhancing SIRT6 activity, the compound induces deacetylation of histone H3 at K9 and K56 positions. In cancer cells, this activation leads to an increase in reactive oxygen species (ROS) levels, which subsequently triggers the AMPK-ULK1-mTOR signaling axis. The ultimate biological outcome is the induction of lethal autophagy and apoptosis. UBCS039 has demonstrated anti-proliferative effects across various tumor models, including non-small cell lung cancer, colorectal cancer, and cervical carcinoma, providing a proof of principle for SIRT6 activation as a potential therapeutic strategy in oncology.

Other names

pyrrolo[1,2-a]quinoxaline derivative