| Name | Apcin |
| 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. |
| 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 : 235 mg/mL (535.73 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (22.8 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (22.8 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
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| Keywords | WD40-domain | ubiquitylation | recognition | pocket | mitosis | ligase | Inhibitor | inhibit | cyclosome | complex | Cdc20 | Apcin | APC/C | APC | anaphase-promoting | Anaphase promoting complex |
| Inhibitors Related | TAME hydrochloride | TASIN-1 | TASIN-1 Hydrochloride | TAME | Bovine Protein C | Apcin A HCL | ProTAME | CFM 4 | Activated Protein C (390-404), human acetate | CP5V | Activated Protein C (390-404), human TFA | CDC20-IN-2 |
| Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library |
United States
