Sirtuin Degrader

SZU-B6 is an orally active SIRT6 PROTAC degrader with DC₅₀ values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells, respectively. SZU-B6 mediates proteasome-dependent degradation of SIRT6 by recruiting the CRBN E3 ubiquitin ligase. SZU-B6 impairs DNA damage repair and promotes radiosensitization of cancer cells. SZU-B6 induces cell cycle arrest and apoptosis in cancer cells. SZU-B6 inhibits the proliferation of liver cancer cells. SZU-B6 suppresses the tumor growth of hepatocellular carcinoma and intrahepatic cholangiocarcinoma in mice. SZU-B6 can be used in research related to hepatocellular carcinoma and intrahepatic cholangiocarcinoma.

Tenovin-3 is a p53 activator.

PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer.