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Description: Apcin is a ligand of Cdc20 and a potent and competitive inhibitor of the E3 ligase activity anaphase-promoting complex/cyclosome (APC/C). It acts by blocking mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe. Apcin competitively inhibits APC/C-dependent ubiquitylation by bindingto Cdc20 and preventing substrate recognition. Apcin occupes theD-box-binding pocket on the side face of the WD40-domain and can prolongmitosis.
References:
1. KatharineL Sackton, et al. Synergistic blockade of mitotic exit by two chemicalinhibitors of the APC/C. Nature. 2014 Oct 30; 514(7524):646-9.
2. KatherineV Richeson, et al. Paradoxical mitotic exit induced by a small moleculeinhibitor of APC/C Cdc20. Nat Chem Biol. 2020 May; 16(5):546-555.
3. SusanneLub, et al. Inhibiting the anaphase promoting complex/cyclosome inducesa metaphase arrest and cell death in multiple myeloma cells.Oncotarget. 2016 Jan 26; 7(4):4062-76.
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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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