[CAS NO. 300815-04-7] Apcin
PRODUCTS SPECIFICATIONS [300815-04-7]
DESCRIPTION [300815-04-7]
Overview
| MDL | MFCD00525727 |
|---|---|
| Molecular Weight | 438.65 |
| Molecular Formula | C13H14Cl3N7O4 |
| SMILES | O=C(OCCN1C([N+]([O-])=O)=CN=C1C)NC(NC2=NC=CC=N2)C(Cl)(Cl)Cl |
2 Publications Citing Use of MCE
Summary
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis [1] [2] [3] .
In Vitro
Apcin (25-50 μM; 48 hours) significantly increases MM apoptosis combining with proTAME (6, 12 μM)
[3]
.
Apcin (25 μM; 2-14 hours) induces slippage more slowly
[2]
.
Apcin (50-200 μM) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects against full-length cyclin B1
[1]
.
Apcin (1.5-200 μM; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mitotic duration in RPE1 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [3]
| Cell Line: | HMCLs LP-1 and RPMI-8226 cells |
| Concentration: | 25, 50 μM |
| Incubation Time: | 48 hours |
| Result: | Had minor effects on multiple myeloma (MM) cells alone and significantly increased MM apoptosis combining with proTAME (6, 12 μM). |
Western Blot Analysis [2]
| Cell Line: | HeLa cells with Nocodazole (100 nM) |
| Concentration: | 25 μM |
| Incubation Time: | 2-14 hours |
| Result: | Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reduction in cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 284.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2797 mL | 11.3986 mL | 22.7972 mL |
| 5 mM | 0.4559 mL | 2.2797 mL | 4.5594 mL |
| 10 mM | 0.2280 mL | 1.1399 mL | 2.2797 mL |
References
- [1] 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.
- [2] 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.
- [3] Susanne Lub, et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76.