Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis[1][2][3].
TAME is an inhibitor of anaphase-promoting complex (APC), which prevents its activation by Cdc20 and Cdh1; TAME is also an inhibitor of cyclin proteolysis in mitotic Xenopus egg extract, with an IC50 of 12 µM.
proTAME is a cell permeable prodrug of TAME, which is an anaphase-promoting complex/cyclosome (APC/C) inhibitor that binds to the APC preferentially suppresses APC/C(Cdc20); arrests cells in metaphase without perturbing the spindle, but is dependent on the spindle assembly checkpoint (SAC); efficiently targets osteosarcoma in vitro combined with chemotherapeutic agents.
TAME hydrochloride is an inhibitor of anaphase-promoting complex (APC), which prevents its activation by Cdc20 and Cdh1.
Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257)[1].