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Apcin

Catalog No. T8561   CAS 300815-04-7

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.

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Apcin Chemical Structure
Apcin, CAS 300815-04-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
2 mg In stock $ 57.00
5 mg In stock $ 89.00
10 mg In stock $ 143.00
25 mg In stock $ 288.00
50 mg In stock $ 497.00
100 mg In stock $ 748.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 96.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 240 mg/mL (547.13 mM), sonification is recommended.

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compound Library Cell Cycle Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Aging Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets
TASIN-1 Hydrochloride TAME TASIN-1 TAME hydrochloride Apcin A HCL Activated Protein C (390-404), human acetate CFM 4

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Keywords

Apcin 300815-04-7 Cell Cycle/Checkpoint APC ligase pocket anaphase-promoting recognition complex Inhibitor Cdc20 Anaphase promoting complex cyclosome ubiquitylation inhibit mitosis WD40-domain APC/C inhibitor

 

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