Art. -Nr.: HY-110287

Apcin

9 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.62%
CAS. Nr.: 300815-04-7
Formel: C₁₃H₁₄Cl₃N₇O₄
Molecular Weight:438.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Apcin Chemical Structure

CAS. Nr.: 300815-04-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

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]

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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 300815-04-7
Appearance Solid
Molecular Weight 438.65
Formel C₁₃H₁₄Cl₃N₇O₄
Color White to off-white
SMILES

O=C(OCCN1C([N+]([O-])=O)=CN=C1C)NC(NC2=NC=CC=N2)C(Cl)(Cl)Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All In Vivo Efficacy StudyIFCell Proliferation/Viability AssayWB

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Journal Impact Factor

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)

The oncogenic role of EIF4A3/CDC20 axis in the endometrial cancer. [Abstract]

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.
Res Sq

2025 Jul 28.
bioRxiv

2025 March 13.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Apcin

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Aging Compound Library Mini

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Apcin

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apcin

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Aging Compound Library Mini

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Apcin

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apcin Related Classifications

HY-110287 Related Classifications