Apcin
Based on 9 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.62%
- No. CAS: 300815-04-7
- Fòrmula: C13H14Cl3N7O4
- Peso molecular:438.65
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Apcin
More- Exp Hematol Oncol. 2023 Aug 1;12(1):67. [Abstract]
- Adv Sci (Weinh). 2026 Mar 2:e16411. [Abstract]
- Adv Sci (Weinh). 2024 Dec;11(45):e2405441. [Abstract]
- EMBO J. 2024 Jun;43(12):2424-2452. [Abstract]
- J Mol Med (Berl). 2024 Nov;102(11):1395-1410. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2023 Feb 9;1869(4):166663. [Abstract]
- Res Sq. 2025 Jul 28.
- bioRxiv. 2025 March 13.
- Bioengineered. 2021 Dec;12(2):10791-10798. [Abstract]
Customer Validation & Images
-
WB
-
IF
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
WB
Actividad biológica
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
193.3 μM
Compound: 5a
|
Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| A549 | IC50 |
>300 μM
Compound: 5a
|
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| A549 | IC50 |
113.61 μM
Compound: Apcin
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
|
[PMID: 38364716] |
| Caov-3 cell line | IC50 |
>300 μM
Compound: 5a
|
Cytotoxicity in human Caov3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human Caov3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| HeLa | IC50 |
220.8 μM
Compound: 5a
|
Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| HepG2 | IC50 |
>300 μM
Compound: 5a
|
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| L02 | IC50 |
>200 μM
Compound: Apcin
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
|
[PMID: 38364716] |
| MCF7 | IC50 |
>300 μM
Compound: 5a
|
Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
| MCF7 | IC50 |
109.36 μM
Compound: Apcin
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
|
[PMID: 38364716] |
| MDA-MB-231 | IC50 |
139.38 μM
Compound: Apcin
|
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
|
[PMID: 38364716] |
| MDA-MB-231 | IC50 |
91.41 μM
Compound: Apcin
|
Cytotoxicity against human TNBC MDA-MB-231 cells assessed as cell viability measured after 72 hrs
Cytotoxicity against human TNBC MDA-MB-231 cells assessed as cell viability measured after 72 hrs
|
[PMID: 35178174] |
| MDA-MB-468 | IC50 |
53.5 μM
Compound: Apcin
|
Cytotoxicity against human TNBC MDA-MB-468 cells assessed as cell viability measured after 72 hrs
Cytotoxicity against human TNBC MDA-MB-468 cells assessed as cell viability measured after 72 hrs
|
[PMID: 35178174] |
| MDA-MB-468 | IC50 |
83.41 μM
Compound: Apcin
|
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay
|
[PMID: 38364716] |
| OVCAR-3 | IC50 |
>300 μM
Compound: 5a
|
Cytotoxicity in human OVCAR3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human OVCAR3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 32290657] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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).
-
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.
Chemical Information
-
No. CAS 300815-04-7
-
Appearance Solid
-
Peso molecular 438.65
-
Fòrmula C13H14Cl3N7O4
-
Color White to off-white
-
SMILES
O=C(OCCN1C([N+]([O-])=O)=CN=C1C)NC(NC2=NC=CC=N2)C(Cl)(Cl)Cl
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
Exp Hematol Oncol
Inhibition of CDC20 potentiates anti-tumor immunity through facilitating GSDME-mediated pyroptosis in prostate cancer. [Abstract]2023 Aug 1;12(1):67. PMID: 37528490
Apcin purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2023 Aug 1;12(1):67. [Abstract]
The schematic graph of experimental design and the picture of xenografts after the sacrifice of mice. Mice bearing TRAMP-C2 tumors implanted 7 days earlier were treated with or without the Cdc20 inhibitor, Apcin (15 mg/kg/d; i.p.; 4 days per cycle for 4 weeks), or the anti-PD1 monoclonal antibodies (5 mice per group). The results showed that the combination of Apcin with α-PD-1 showed prominent therapeutic superiority to α-PD-1 alone (P < 0.01) and to Apcin alone (P < 0.01).
-
Adv Sci (Weinh)
GNL3 Orchestrates AR Transcriptional Programs to Drive Castration-Resistant Prostate Cancer and Immune Evasion. [Abstract]2026 Mar 2:e16411. PMID: 41772945 -
Adv Sci (Weinh)
The Tumor Suppressor TPD52-Governed Endoplasmic Reticulum Stress is Modulated by APCCdc20. [Abstract]2024 Dec;11(45):e2405441. PMID: 39401430
Apcin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec;11(45):e2405441. [Abstract]
IB analysis of TPD52 and Cdc20 expression in T24 cells treated with Apcin at the indicated concentrations for 24 hours or treated with Apcin (20 μM) for indicated time (6, 12 and 24 hours).
-
EMBO J
A non-canonical role of the inner kinetochore in regulating sister-chromatid cohesion at centromeres. [Abstract]2024 Jun;43(12):2424-2452. PMID: 38714893
Apcin purchased from MedChemExpress. Usage Cited in: EMBO J. 2024 Jun;43(12):2424-2452. [Abstract]
HeLa cells were transfected with control siRNA or CENP-U siRNA. At 48 h post-transfection, cells were treated with Apcin (250 μM) for 6 h, then mitotic chromosome spreads were prepared, stained.
-
J Mol Med (Berl)
2024 Nov;102(11):1395-1410. PMID: 39316093
Apcin purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2024 Nov;102(11):1395-1410. [Abstract]
The IC50 assay was used to detect the inhibitory efficacy of Apcin (48 h) in EIF4A3 overexpressing cell lines. Data are shown as the mean ± SD (n = 3). The results showed that overexpression of EIF4A3 downregulated the Apcin IC50 in Ishikawa cells (90.48 μM vs 140.2 μM) and HEC-1-A cells (142.5 μM vs 196.9 μM).
-
Biochim Biophys Acta Mol Basis Dis
CDC20 inhibition alleviates fibrotic response of renal tubular epithelial cells and fibroblasts by regulating nuclear translocation of β-catenin. [Abstract]2023 Feb 9;1869(4):166663. PMID: 36764621
Apcin purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2023 Feb 9;1869(4):166663. [Abstract]
Apcin (5 mg/kg; i.p.; once daily for 7 days) significantly attenuated both Collagen I and Collagen III in a renal fibrosis animal model (unilateral ureteral obstruction, UUO), and decreaseed the level of profibrotic factor TGF-β1.
-
-
-
Bioengineered
Apcin inhibits the growth and invasion of glioblastoma cells and improves glioma sensitivity to temozolomide. [Abstract]2021 Dec;12(2):10791-10798. PMID: 34753395
Solvente y solubilidad
DMSO : 100 mg/mL (227.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2797 mL | 11.3986 mL | 22.7972 mL | 56.9930 mL |
| 5 mM | 0.4559 mL | 2.2797 mL | 4.5594 mL | 11.3986 mL | |
| 10 mM | 0.2280 mL | 1.1399 mL | 2.2797 mL | 5.6993 mL | |
| 15 mM | 0.1520 mL | 0.7599 mL | 1.5198 mL | 3.7995 mL | |
| 20 mM | 0.1140 mL | 0.5699 mL | 1.1399 mL | 2.8497 mL | |
| 25 mM | 0.0912 mL | 0.4559 mL | 0.9119 mL | 2.2797 mL | |
| 30 mM | 0.0760 mL | 0.3800 mL | 0.7599 mL | 1.8998 mL | |
| 40 mM | 0.0570 mL | 0.2850 mL | 0.5699 mL | 1.4248 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4559 mL | 1.1399 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3800 mL | 0.9499 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2850 mL | 0.7124 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5699 mL |
Apcin Related Classifications
HY-110287 Related Classifications
Powered by Bioz