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Apcin is a potent and competitive inhibitor of anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. It acts by blocking mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $40 | In Stock | |
| 2 mg | $57 | In Stock | |
| 5 mg | $89 | In Stock | |
| 10 mg | $143 | In Stock | |
| 25 mg | $288 | In Stock | |
| 50 mg | $497 | In Stock | |
| 100 mg | $748 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock |
| Description | Apcin is a potent and competitive inhibitor of anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. It acts by blocking mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe. |
| In vitro | apcin as a small molecule ligand of Cdc20 that inhibits APC/CCdc20 and prolongs mitosis.?apcin paradoxically shortens mitosis when SAC activity is high.?These opposing effects of apcin arise from targeting of a common binding site in Cdc20 required for both substrate ubiquitination and MCC-dependent APC/C inhibition.?Furthermore, apcin cooperates with p31comet to relieve MCC-dependent inhibition of APC/C.?Apcin therefore causes either net APC/C inhibition, prolonging mitosis when SAC activity is low, or net APC/C activation, shortening mitosis when SAC activity is high, demonstrating that a small molecule can produce opposing biological effects depending on regulatory context. |
| Molecular Weight | 438.65 |
| Formula | C13H14Cl3N7O4 |
| Cas No. | 300815-04-7 |
| Smiles | Cc1ncc(n1CCC(=O)NC(Nc1ccccc1)C(Cl)(Cl)Cl)[N+]([O-])=O |
| Relative Density. | 1.68 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 240 mg/mL (547.13 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.4 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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