Aphidicolin
Based on 15 publication(s) in Google Scholar
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
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- Purity: 99.93%
- CAS No.: 38966-21-1
- 화학식: C20H34O4
- 분자량:338.48
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Aphidicolin
More- Cell. 2025 Jun 26;188(13):3405-3421.e27. [Abstract]
- Cell. 2024 Jul 25;187(15):3936-3952.e19. [Abstract]
- Nat Commun. 2023 May 26;14(1):3050. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1182-1193. [Abstract]
- Nucleic Acids Res. 2024 Feb 9;52(3):1136-1155. [Abstract]
- Cell Death Dis. 2026 Feb 3;17(1):201. [Abstract]
- Dev Cell. 2025 Jun 25:S1534-5807(25)00362-4. [Abstract]
- Int Endod J. 2025 Sep 23. [Abstract]
- Cell Rep. 2025 Jan 16;44(1):115215. [Abstract]
- Antiviral Res. 2020 Nov;183:104931. [Abstract]
- bioRxiv. 2026 Mar 13.
- bioRxiv. 2025 Sep 21.
- bioRxiv. 2025 May 3:2025.04.29.650984. [Abstract]
- University of Zurich. 2025 Feb 04.
- bioRxiv. 2024 August 31.
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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RT-PCR
All DNA/RNA Synthesis Isoforms
MoreAll Antibiotic Isoforms
More
Biological Activity
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DNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
9 μM
Compound: Aphidicolin
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Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 24 hrs by WST-1 assay
Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 24 hrs by WST-1 assay
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[PMID: 24926891] |
| HFF | IC50 |
0.473 μM
Compound: Aphidicolin
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Inhibition of VZV KOS DNA polymerase infected in HFF cells
Inhibition of VZV KOS DNA polymerase infected in HFF cells
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[PMID: 20403696] |
| HFF | IC50 |
0.487 μM
Compound: Aphidicolin
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Inhibition of HCMV DNA polymerase infected in HFF cells
Inhibition of HCMV DNA polymerase infected in HFF cells
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[PMID: 20403696] |
| HL-60 | IC50 |
24.4 μM
Compound: Aphidicolin
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Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 31403790] |
| P388 | ED50 |
0.13 μg/mL
Compound: 1, aphidicolin
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In vivo antitumor activity against mouse P388 cells
In vivo antitumor activity against mouse P388 cells
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[PMID: 6434698] |
| Sf9 | IC50 |
473 nM
Compound: Aphidicolin
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Inhibition of Varicella zoster virus recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay
Inhibition of Varicella zoster virus recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay
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[PMID: 20167488] |
| Sf9 | IC50 |
487 nM
Compound: Aphidicolin
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Inhibition of HCMV recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay
Inhibition of HCMV recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay
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[PMID: 20167488] |
| Vero | CC50 |
0.2 mg/mL
Compound: 1
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Cytotoxicity against african green monkey Vero cells after 66 hrs
Cytotoxicity against african green monkey Vero cells after 66 hrs
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[PMID: 1667410] |
| Vero | IC50 |
0.438 μM
Compound: Aphidicolin
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Inhibition of HSV1 KOS DNA polymerase infected in african green monkey Vero cells
Inhibition of HSV1 KOS DNA polymerase infected in african green monkey Vero cells
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[PMID: 20403696] |
| Vero | IC50 |
0.58 μM
Compound: Aphidicolin
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Cytotoxicity against african green monkey Vero cells assessed as loss of monolayer present around the plaques
Cytotoxicity against african green monkey Vero cells assessed as loss of monolayer present around the plaques
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[PMID: 20691339] |
| Vero | IC50 |
0.58 μM/L
Compound: Aphidicolin
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Cytotoxicity against african green monkey Vero cells assessed as loss of monolayer present around the plaques
Cytotoxicity against african green monkey Vero cells assessed as loss of monolayer present around the plaques
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[PMID: 20691339] |
Aphidicolin (0.5 μM, 5 μM; 0-5 d) selectively kills neuroblastoma cells, but shows moderate cytotoxicity on normal human embryonal cells and HeLa, H9, A549 and Caco-2 cell lines[4].
Aphidicolin (0.4 μg/mL; 3 d) arrests cell cycle at G2 phase[5].
Aphidicolin (100 nM-10 μM; 48 h) inhibits cell proliferation via the p53-GADD45β pathway and (1 μM; 24 h) induces apoptosis in AtT-20 cells[6].
Aphidicolin (10 μM; 0-6 h) decreases the phosphorylation of Akt, (100 nM-10 μM; 24 h) increases the mRNA levels of the stress response gene growth arrest and DNA damage-inducible 45β (GADD45β), a putative downstream target of p53[6].
Aphidicolin (10 μM; 0-6 h) inhibits Varicella-zoster virus (VZV) with EC50s of 0.5-0.6 μM, with low cytotoxicity[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NB cell lines: UKF-NB-1/2/3 and IMR-32
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Concentration:0.5 μM, 5μM
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Incubation Time:1, 2, 3, 4, 5 days
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Result:Resulted in cellular enlargement and extension of cellular processes before cell lysis occurred.
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Cell Line:Normal human diploid cells
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Concentration:0.4 μg/mL
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Incubation Time:3 days or 7 days
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Result:Resulted more than 80% of the cells moved through S phase and were accumulated at G2 phase.
Inbihited the growth of the cells completely without causing apparent cell death.
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Cell Line:AtT-20 cells pituitary corticotroph tumor cells
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Concentration:10 µM
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Incubation Time:0 min, 5 min, 30 min, 2 h, 6 h, 24 h
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Result:Inhibited Akt phosphorylation in AtT-20 cells during 5 min-2 h, in a time-dependent manner.
Increased protein level of p27 during 30 min-6 h, and remarkably increased p53 level at 24 h.
Aphidicolin glycinate (100 mg/kg; i.p.; once every 3 h; 9 d) shows anti-tumor activity against the implanted B16 melanoma and M5076 sarcoma in murine, producing maximum increased life spans of 75%[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:M5076 sarcoma s.c. model or B16 melanoma i.p. model in murine[8]
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Dosage:60 mg/kg, 100 mg/kg, 300 mg/kg
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Administration:Intraperitoneal injection; once every 3 h; 9 days
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Result:Inhibited tumor growth significantly.
Chemical Information
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CAS No. 38966-21-1
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Appearance Solid
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분자량 338.48
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화학식 C20H34O4
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Color White to off-white
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SMILES
C[C@@]12[C@]34[C@](CC[C@@]1([H])[C@@](C)([C@H](O)CC2)CO)([H])C[C@]([C@](CO)(O)CC4)([H])C3
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Structure Classification
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Initial Source
Cephalosporium aphidicola
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (15)
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Journal Impact Factor
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Most Recent
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Cell
Extrachromosomal DNA replication and maintenance couple with DNA damage pathway in tumors. [Abstract]2025 Jun 26;188(13):3405-3421.e27. PMID: 40300601 -
Cell
Amplification editing enables efficient and precise duplication of DNA from short sequence to megabase and chromosomal scale. [Abstract]2024 Jul 25;187(15):3936-3952.e19. PMID: 38936359
Aphidicolin purchased from MedChemExpress. Usage Cited in: Cell. 2024 Jul 25;187(15):3936-3952.e19. [Abstract]
The synthesis of new DNA in RPE-1 cells was detected by EdU incorporation assay at 6, 12, 24, 48 and 72 hours after treatment with the drug Aphidicolin (2 μg/mL).
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Nat Commun
TRABID inhibition activates cGAS/STING-mediated anti-tumor immunity through mitosis and autophagy dysregulation. [Abstract]2023 May 26;14(1):3050. PMID: 37237031
Aphidicolin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 26;14(1):3050. [Abstract]
Westernblot analysis of TRABID mRNA and protein levels in HeLa cells treated with 10 μM Lovastatin, 2 μg/ml Aphidicolin, 10 μM RO-3306, or 3 μM Nocodazole for 18 h.
Aphidicolin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 26;14(1):3050. [Abstract]
RT-qPCR analysis of TRABID mRNA and protein levels in HeLa cells treated with 10 μM Lovastatin, 2 μg/ml Aphidicolin, 10 μM RO-3306, or 3 μM Nocodazole for 18 h.
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Nat Chem Biol
2025 Aug;21(8):1182-1193. PMID: 39809895
Aphidicolin purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 Aug;21(8):1182-1193. [Abstract]
Clonal survival analysis of MSANTD4-deficient U2OS cells after treatment with Aphidicolin (0-600 nM; 24 h).
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Nucleic Acids Res
DAXX promotes centromeric stability independently of ATRX by preventing the accumulation of R-loop-induced DNA double-stranded breaks. [Abstract]2024 Feb 9;52(3):1136-1155. PMID: 38038252 -
Cell Death Dis
2026 Feb 3;17(1):201. PMID: 41633992 -
Dev Cell
Conserved signals control self-organization and symmetry breaking of murine bilayered epithelia during development and regeneration. [Abstract]2025 Jun 25:S1534-5807(25)00362-4. PMID: 40592344 -
Int Endod J
Long-Term Biobanked Dental Pulp Stem Cells Retain Angiogenic Potential for Vascularised Tissue Engineering-Laboratory Investigation. [Abstract]2025 Sep 23. PMID: 40988150 -
Cell Rep
Deciphering transcription activity of mammalian early embryos unveils on/off of zygotic genome activation by protein translation/degradation. [Abstract]2025 Jan 16;44(1):115215. PMID: 39823229 -
Antiviral Res
Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: Efficacy of decitabine and valganciclovir alone or in combination. [Abstract]2020 Nov;183:104931. PMID: 32926887 -
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Aphidicolin purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Sep 21.
The scatter plot shows the number of TOPBP1 aggregation foci per mitotic cell in U2OS cells treated with Aphidicolin (0.4 μM) for 24 hours after siRNA depletion.
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bioRxiv
2025 May 3:2025.04.29.650984. PMID: 40568099 -
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용액&용해도
DMSO : 100 mg/mL (295.44 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (7.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (282 KB)
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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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Dresler SL, et al. Involvement of DNA polymerase delta in DNA repair synthesis in human fibroblasts at late times after ultraviolet irradiation. Biochemistry. 1988 Aug 23;27(17):6379-83. [Content Brief]
[2]. Bucknall RA, et al. Antiviral effects of aphidicolin, a new antibiotic produced by Cephalosporium aphidicola. Antimicrob Agents Chemother. 1973 Sep;4(3):294-8. [Content Brief]
[3]. Kuwakado K, et al. Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemiacell lines. Biochem Pharmacol. 1993 Dec 3;46(11):1909-16. [Content Brief]
[4]. Cinatl J, et al. Aphidicolin selectively kills neuroblastoma cells in vitro. Cancer Lett. 1992 Dec 24;67(2-3):199-206. [Content Brief]
[5]. Kageyama K, et al. Aphidicolin inhibits cell proliferation via the p53-GADD45β pathway in AtT-20 cells. Endocr J. 2015;62(7):645-54. [Content Brief]
[6]. Fukuda M, Ohashi M. Aphidicolin inhibits cell growth by accumulation of G2 cells. Cell Biol Int Rep. 1983 Aug;7(8):579-85. [Content Brief]
[7]. Rowe J, et al. Compounds that target host cell proteins prevent varicella-zoster virus replication in culture, ex vivo, and in SCID-Hu mice. Antiviral Res. 2010 Jun;86(3):276-85. [Content Brief]
[8]. O'Dwyer PJ, et al. Antitumor activity and biochemical effects of aphidicolin glycinate (NSC 303812) alone and in combination with cisplatin in vivo. Cancer Res. 1994 Feb 1;54(3):724-9. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9544 mL | 14.7719 mL | 29.5438 mL | 73.8596 mL |
| 5 mM | 0.5909 mL | 2.9544 mL | 5.9088 mL | 14.7719 mL | |
| 10 mM | 0.2954 mL | 1.4772 mL | 2.9544 mL | 7.3860 mL | |
| 15 mM | 0.1970 mL | 0.9848 mL | 1.9696 mL | 4.9240 mL | |
| 20 mM | 0.1477 mL | 0.7386 mL | 1.4772 mL | 3.6930 mL | |
| 25 mM | 0.1182 mL | 0.5909 mL | 1.1818 mL | 2.9544 mL | |
| 30 mM | 0.0985 mL | 0.4924 mL | 0.9848 mL | 2.4620 mL | |
| 40 mM | 0.0739 mL | 0.3693 mL | 0.7386 mL | 1.8465 mL | |
| 50 mM | 0.0591 mL | 0.2954 mL | 0.5909 mL | 1.4772 mL | |
| 60 mM | 0.0492 mL | 0.2462 mL | 0.4924 mL | 1.2310 mL | |
| 80 mM | 0.0369 mL | 0.1846 mL | 0.3693 mL | 0.9232 mL | |
| 100 mM | 0.0295 mL | 0.1477 mL | 0.2954 mL | 0.7386 mL |
- Aphidicolin
- 38966-21-1
- DNA/RNA Synthesis
- HSV
- Apoptosis
- Antibiotic
- Orthopoxvirus
- promyelocytic leukemia cell
- cellular deoxyribonucleic acid synthesis
- herpes simplex virus
- DNA polymerase
- mitotic cell division
- anti-orthopoxvirus
- arabinosyl nucleosides
- neuroblastoma cells
- cell killing
- ACTH
- POMC
- pituitary
- Cushing’s disease
- pituitary corticotroph tumor cells
- Inhibitor
- inhibitor
- inhibit