Apcin, a ligand for Cdc20, is a potent, competitive inhibitor of APC/C(Cdc20) Apcin competitively inhibits APC/C-dependent ubiquitination by binding to Cdc20 and preventing substrate recognition. Apcin occupies the D-box binding pocket flanking the WD40 structural domain, which prolongs mitosis[1][2][3].At concentrations of 25-50 μM for 48 hours, Apcin in combination with proTAME (6, 12 μM) significantly increases MM apoptosis[3].At 25 μM concentration, acting for 2-14 hours, Apcin induces slippage at a slower rate[2].In the concentration range of 50-200 μM, Apcin most effectively stabilises cycB1-NT and securin, with a slightly weaker effect on full-length cyclin B1[1].In the concentration range of 1.5-200 μM for 18 hours, Apcin acts synergistically with proTAME, a cell-permeable TAME prodrug, to prolong the mitotic duration of RPE1 cells[1].
Apcin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
H9C2 cells
2 μM
24 h
To assess the potential damage of DOX to cardiomyocytes, observed vacuolization and reduction in cell count.
Cell Mol Biol Lett. 2025 Mar 5;30(1):29.
JVM2 cells
50 μM, 100 μM, 200 μM
24h, 48h, 72h
Inhibit cell proliferation, migration and invasion, induce cell apoptosis and cell cycle arrest
Exp Hematol Oncol. 2023 Mar 7;12(1):28.
Z138 cells
50 μM, 100 μM, 200 μM
24h, 48h, 72h
Inhibit cell proliferation, migration and invasion, induce cell apoptosis and cell cycle arrest
Exp Hematol Oncol. 2023 Mar 7;12(1):28.
RPE1 cells
25 μM
45 h
To evaluate the effects of apcin and proTAME on mitotic duration. Results showed that apcin and proTAME synergistically prolonged mitotic duration.
Nature. 2014 Oct 30;514(7524):646-9.
cells in mitotic Xenopus egg extract
200 μM
40 min
To evaluate the effects of apcin and its derivatives on the degradation of the N-terminal fragment of cyclin B1. Results showed that apcin effectively inhibited degradation.
Nature. 2014 Oct 30;514(7524):646-9.
HCT116 cells
50 μM
24 h
To determine the effect of apcin on cyclin B1 degradation, results showed that apcin accelerated cyclin B1 degradation.
Nat Chem Biol. 2020 May;16(5):546-555.
hTERT-RPE1 H2B-GFP cells
0, 3.1, 6.2, 12.5, 25, 50 μM
24 h
To determine the effect of apcin on mitotic fraction, results showed that apcin dose-dependently decreased the mitotic fraction.
Nat Chem Biol. 2020 May;16(5):546-555.
PC3 cells
50 µM
48 h
To evaluate the effect of Apcin on PC3 cell viability and apoptosis, results showed that Apcin reduced cell viability and induced apoptosis in a dose-dependent manner
Cancer Lett. 2017 Jan 28;385:207-214.
Apcin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
TRAMP-C2 subcutaneous tumor model
Intraperitoneal injection
15 mg/kg
Once daily ,4 days per cycle
To evaluate the anti-tumor effect of Apcin combined with anti-PD1 antibodies
Exp Hematol Oncol. 2023 Aug 1;12(1):67
C57BL/6 mice
DOX-induced myocardial injury model
Intraperitoneal injection
1.5 mg/kg
Once daily for 4 weeks
To evaluate the effect of CDC20 inhibitor Apcin on DOX-induced myocardial injury, found that Apcin exacerbated cardiomyocyte apoptosis.
Cell Mol Biol Lett. 2025 Mar 5;30(1):29.
Balb/c nude mice
Z138 cell-driven xenograft tumor model
Intraperitoneal injection
20 mg/kg
Every other day for 2 weeks
Evaluate the anti-tumor effect and safety of Apcin in vivo
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