Apcin - CAS 300815-04-7
Category: Inhibitor
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Apcin is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C), which is a large multimeric complex. It functions as a ubiquitin ligase, initiating the metaphase-anaphase transition and regulating ordered transitions through the cell cycle by controlling the ubiquitin-mediated proteolysis of cell cycle proteins. It competitively binds to the D-box binding site of Cdc20 and prevents substrate recognition and ubiquitylation required for continuation of mitosis. It synergistically increases apoptosis in multiple myeloma cells in combination with proTAME (prodrug of TAME). It also prolongs mitotic duration in RPE1 cells in combination with proTAME in vitro. It blocks mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe.
≥98% by HPLC
3-(2-Methyl-5-nitro-imidazol-1-yl)-N-(2,2,2-trichloro-1-phenylamino-ethyl)-propionamide; 2-(2-Methyl-5-nitroimidazol-1-yl)ethyl N-[2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl]carbamate; [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-carbamic acid, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester
Canonical SMILES:
1.Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells.
Lub S;Maes A;Maes K;De Veirman K;De Bruyne E;Menu E;Fostier K;Kassambara A;Moreaux J;Hose D;Leleu X;King RW;Vanderkerken K;Van Valckenborgh E Oncotarget. 2016 Jan 26;7(4):4062-76. doi: 10.18632/oncotarget.6768.
The anaphase promoting complex/cyclosome (APC/C) is an ubiquitin ligase involved in cell cycle. During the metaphase-anaphase transition the APC/C is activated by Cdc20. The aim of this study is to elucidate the importance and therapeutic potential of APC/C and its co-activator Cdc20 in multiple myeloma (MM). Gene expression analysis revealed that Cdc20 was expressed at higher levels in gene expression-based high-risk MM patients. Moreover, high Cdc20 expression correlated with poor prognosis. Treatment of human myeloma cell lines with proTAME, an APC/C inhibitor, resulted in an accumulation of APC/CCdc20 substrate cyclin B1 and an accumulation of cells in metaphase. Moreover we observed a significant dose-dependent decrease in viability and increase in apoptosis in MM cells upon proTAME treatment. The induction of apoptosis was accompanied with caspase 3, 8, 9 and PARP cleavage. A similar metaphase arrest and induction of apoptosis were obtained with specific knockdown of Cdc20. In addition, we demonstrated the accumulation of Bim was partially responsible for the observed cell death. Combining proTAME with another APC/C inhibitor apcin or the alkylating agent melphalan resulted in enhanced anti-MM activity.
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