Apcin-A

Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287) . Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257) [1][2][3].

Product Specifications

CAS Number

[1683617-62-0]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

APC; Ligands for Target Protein for PROTAC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/apcin-a.html

Purity

98.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(OCCCN)NC(NC1=NC=CC=N1)C(Cl)(Cl)Cl

Molecular Formula

C10H14Cl3N5O2

Molecular Weight

342.61

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Richeson KV, et al. Paradoxical mitotic exit induced by a small molecule inhibitor of APC/CCdc20. Nat Chem Biol. 2020 May;16 (5) :546-555.|[2]Sackton KL, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct 30;514 (7524) :646-9.|[3]Chi JJ, et al. A novel strategy to block mitotic progression for targeted therapy. EBioMedicine. 2019 Oct 25. pii: S2352-3964 (19) 30677-2.