Apcin |
Catalog No.GC18518
One-Click Copy Product Info
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Apcin is a small cell-permeable APC/C inhibitor that blocks the interaction between APC/C and Cdc20 or Cdh1, with a KD value of 236µM for Cdc20.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 300815-04-7
Sample solution is provided at 25 µL, 10mM.
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Apcin is a small cell-permeable APC/C inhibitor that blocks the interaction between APC/C and Cdc20 or Cdh1, with a KD value of 236µM for Cdc20[1]. Apcin occupies the D-box-binding pocket on the side face of the WD40-domain of Cdc20 protein, competitively inhibiting binding of Cdc20 to the ubiquitylation of D-box-containing substrates[2]. Apcin has been widely used in mitosis research to induce lethal mitotic arrest and cell death[3].
In vitro, Apcin treatment for 48 hours significantly inhibited the viability of A375 and HeLa cells, with IC50 values of 193.3µM and 220.8µM, respectively[4]. Incubating MG63 and U2OS cells with 75µM Apcin for 48 hours induced apoptosis, accompanied by an increase in the expression of pro-apoptotic molecules Bim and p21[5]. Treatment with 100µM Apcin for 48 hours suppressed the migration and proliferation of Z138 cells, promoted G2/M phase arrest of the cells, and reduced the expression of MMP2 and MMP9[6].
In vivo, Apcin treatment via intraperitoneal injection at a dose of 5mg/kg/day for 5 days alleviated the renal dysfunction and tubular damage in mice with acute kidney injury induced by cisplatin[7]. In a unilateral urinary tract obstruction mouse model, intraperitoneal injection of Apcin (1mg/kg/day) for 8 consecutive days reduced collagen deposition and fibrotic lesions in the renal interstitium and inhibited the expression of inflammatory factors[8]. Intraperitoneal injection of Apcin at a dose of 30μM/kg, every other day for 16 consecutive days, markedly suppressed tumor growth in KLE xenograft mice without affecting body weight[9].
References:[1] He Y, Le X, Hu G, et al. Discovery of ureido-based apcin analogues as Cdc20-specific inhibitors against cancer[J]. Pharmaceuticals, 2023, 16(2): 304.
[2] Sackton K L, Dimova N, Zeng X, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C[J]. Nature, 2014, 514(7524): 646-649.
[3] De Lange J, Faramarz A, Oostra A B, et al. Defective sister chromatid cohesion is synthetically lethal with impaired APC/C function[J]. Nature communications, 2015, 6(1): 8399.
[4] Huang P, Le X, Huang F, et al. Discovery of a dual tubulin polymerization and cell division cycle 20 homologue inhibitor via structural modification on apcin[J]. Journal of Medicinal Chemistry, 2020, 63(9): 4685-4700.
[5] Gao Y, Zhang B, Wang Y, et al. Cdc20 inhibitor apcin inhibits the growth and invasion of osteosarcoma cells[J]. Oncology reports, 2018, 40(2): 841-848.
[6] Chen Y, Yang P, Gao S, et al. Inhibition of CDC20 suppresses the development and progression of mantle cell lymphoma through PI3K/AKT pathway[J]. Annals of Hematology, 2026, 105(4): 169.
[7] You R, Li Y, Jiang Y, et al. WWP2 deletion aggravates acute kidney injury by targeting CDC20/autophagy axis[J]. Journal of Advanced Research, 2025, 71: 471-485.
[8] He J, Xu S, Jiang M, et al. CDC20 inhibition alleviates fibrotic response of renal tubular epithelial cells and fibroblasts by regulating nuclear translocation of β-catenin[J]. Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 2023, 1869(4): 166663.
[9] Ni K, Li Z, Hu Z, et al. Antitumor effect of apcin on endometrial carcinoma via p21-mediated cell cycle arrest and apoptosis[J]. Current Medical Science, 2024, 44(3): 623-632.
| Cell experiment [1]: | |
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Cell lines |
A375 cells |
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Preparation Method |
A375 cells were cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum, 1% glutamine, 100U/ml penicillin, and 100μg/ml streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in triplicate into 96-well plates (5×103 cells/well) and allowed to adhere overnight. Cells were incubated with Apcin at various concentrations (0.03, 0.1, 0.33, 1, 10, 100, 200, and 300μM) for 48h, and cell viability was tested. |
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Reaction Conditions |
0.03, 0.1, 0.33, 1, 10, 100, 200, and 300μM; 48h |
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Applications |
Apcin treatment decreased cell viability of A375 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c nude mice |
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Preparation Method |
Female BALB/c nude mice (4 weeks old) were housed in SPF conditions with an automatic 12h/12h light-dark cycle at a constant temperature (21±1°C). KLE cells (1×107) were injected subcutaneously into the right flank of nude mice. Three weeks later, the tumor-bearing mice were randomly assigned to the vehicle control group or the Apcin group. The mice in the control group and the Apcin group were injected intraperitoneally with PBS and 30μM/kg Apcin, respectively, every other day for 16 days. The body weight and tumor size were measured every 4 days. Tumor volume (cm3) was calculated using the formula (length×width×width)/2. |
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Dosage form |
30μM/kg; every other day; 16 days; i.p. |
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Applications |
Apcin treatment reduced tumor growth in the KLE xenograft mouse model. |
| References: [1] Huang P, Le X, Huang F, et al. Discovery of a dual tubulin polymerization and cell division cycle 20 homologue inhibitor via structural modification on apcin[J]. Journal of Medicinal Chemistry, 2020, 63(9): 4685-4700. [2] Ni K, Li Z, Hu Z, et al. Antitumor effect of apcin on endometrial carcinoma via p21-mediated cell cycle arrest and apoptosis[J]. Current Medical Science, 2024, 44(3): 623-632. | |
| Cas No. | 300815-04-7 | SDF | |
| Chemical Name | [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-carbamic acid, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester | ||
| Canonical SMILES | CC1=NC=C([N+]([O-])=O)N1CCOC(NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)=O | ||
| Formula | C13H14Cl3N7O4 | M.Wt | 438.7 |
| Solubility | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2795 mL | 11.3973 mL | 22.7946 mL |
| 5 mM | 455.9 μL | 2.2795 mL | 4.5589 mL |
| 10 mM | 227.9 μL | 1.1397 mL | 2.2795 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)