Apcin

SKU: orb1298832

Description

Apcin is a potent, competitive inhibitor of the APC/C-Cdc20 E3 ligase, binding Cdc20 to block substrate recognition and ubiquitination. This inhibition arrests cells in mitosis and is synergistically enhanced by Ts-Arg-OMe, making it a valuable tool for studying cell cycle regulation, mitotic exit, and aneuploidy in both cellular and biochemical assays.

Research Area

Cell Biology

Key Properties

• CAS Number: 300815-04-7
• MW: 438.65
• Purity: 96.48% (May vary between batches)
• Formula: C₁₃H₁₄Cl₃N₇O₄
• SMILES: Cc1ncc(n1CCC(=O)NC(Nc1ccccc1)C(Cl)(Cl)Cl)[N+]([O-])=O
• Target: APC/C
• Solubility: DMSO:235 mg/mL (535.73 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.4 mM)

Bioactivity

• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

mitosis, inhibit, ligase, Inhibitor, cyclosome, complex, Cdc20, Apcin, APC/C, APC, anaphase-promoting, Anaphase promoting complex, pocket, recognition, WD40-domain, ubiquitylation

Compound Identifiers

PubChem CID

91895229