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Apcin

  Cat. No.:  DC20310   Featured
Chemical Structure
300815-04-7
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Field of application
Apcin is a cell-permeable, small molecule anaphase-promoting complex/cyclosome (APC/C) inhibitor, which binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 300815-04-7
Chemical Name: [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-carbamic acid, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester
SMILES: O=C(NC(C(Cl)(Cl)Cl)NC1=NC=CC=N1)OCCN1C(C)=NC=C1[N+]([O-])=O
Formula: C13H14Cl3N7O4
M.Wt: 438.65
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
In Vitro: Apcin (25-50 μM; 48 hours) significantly increases MM apoptosis combining with proTAME (6, 12 μM)[3]. Apcin (25 μM; 2-14 hours) induces slippage more slowly[2]. Apcin (50-200 μM) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects against full-length cyclin B1[1]. Apcin (1.5-200 μM; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mitotic duration in RPE1 cells[1]. Apoptosis Analysis[3] Cell Line: HMCLs LP-1 and RPMI-8226 cells Concentration: 25, 50 μM Incubation Time: 48 hours Result: Had minor effects on multiple myeloma (MM) cells alone and significantly increased MM apoptosis combining with proTAME (6, 12 μM). Western Blot Analysis[2] Cell Line: HeLa cells with Nocodazole (100 nM) Concentration: 25 μM Incubation Time: 2-14 hours Result: Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reduction in cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry.
References: [1]. Katharine L Sackton, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct 30;514(7524):646-9. [2]. Katherine V Richeson, et al. Paradoxical mitotic exit induced by a small molecule inhibitor of APC/C Cdc20. Nat Chem Biol. 2020 May;16(5):546-555. [3]. Susanne Lub, et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76.
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