Art. -Nr.: HY-N6733

Aphidicolin

15 Cited Publications

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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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Reinheit: 99.93%
CAS. Nr.: 38966-21-1
Formel: C₂₀H₃₄O₄
Molecular Weight:338.48

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Aphidicolin Chemical Structure

CAS. Nr.: 38966-21-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

DNA Polymerase

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Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	9 μM Compound: Aphidicolin	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	[PMID: 24926891]
HFF	IC₅₀	0.473 μM Compound: Aphidicolin	Inhibition of VZV KOS DNA polymerase infected in HFF cells Inhibition of VZV KOS DNA polymerase infected in HFF cells	[PMID: 20403696]
HFF	IC₅₀	0.487 μM Compound: Aphidicolin	Inhibition of HCMV DNA polymerase infected in HFF cells Inhibition of HCMV DNA polymerase infected in HFF cells	[PMID: 20403696]
HL-60	IC₅₀	24.4 μM Compound: Aphidicolin	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	[PMID: 31403790]
P388	ED₅₀	0.13 μg/mL Compound: 1, aphidicolin	In vivo antitumor activity against mouse P388 cells In vivo antitumor activity against mouse P388 cells	[PMID: 6434698]
Sf9	IC₅₀	473 nM Compound: Aphidicolin	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	[PMID: 20167488]
Sf9	IC₅₀	487 nM Compound: Aphidicolin	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	[PMID: 20167488]
Vero	CC₅₀	0.2 mg/mL Compound: 1	Cytotoxicity against african green monkey Vero cells after 66 hrs Cytotoxicity against african green monkey Vero cells after 66 hrs	[PMID: 1667410]
Vero	IC₅₀	0.438 μM Compound: Aphidicolin	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	[PMID: 20403696]
Vero	IC₅₀	0.58 μM Compound: Aphidicolin	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	[PMID: 20691339]
Vero	IC₅₀	0.58 μM/L Compound: Aphidicolin	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	[PMID: 20691339]

In Vitro

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.

Cell Cytotoxicity Assay^[4]

Cell Line:

NB cell lines: UKF-NB-1/2/3 and IMR-32
Concentration:

0.5 μM, 5μM
Incubation Time:

1, 2, 3, 4, 5 days
Result:

Resulted in cellular enlargement and extension of cellular processes before cell lysis occurred.

Cell Cycle Analysis^[5]

Cell Line:

Normal human diploid cells
Concentration:

0.4 μg/mL
Incubation Time:

3 days or 7 days
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.

Western Blot Analysis^[6]

Cell Line:

AtT-20 cells pituitary corticotroph tumor cells
Concentration:

10 µM
Incubation Time:

0 min, 5 min, 30 min, 2 h, 6 h, 24 h
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.

In Vivo

Aphidicolin, has been developed with higher solubility agent, namely Aphidicolin glycinate (AG; NSC 303812).
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.

Animal Model:

M5076 sarcoma s.c. model or B16 melanoma i.p. model in murine^[8]
Dosage:

60 mg/kg, 100 mg/kg, 300 mg/kg
Administration:

Intraperitoneal injection; once every 3 h; 9 days
Result:

Inhibited tumor growth significantly.

Chemical Information

CAS. Nr. 38966-21-1
Appearance Solid
Molecular Weight 338.48
Formel C₂₀H₃₄O₄
Color White to off-white
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
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
- Microorganisms
Cephalosporium aphidicola
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (15)

All Cell Proliferation/Viability AssayWBRT-PCR

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Journal Impact Factor

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).
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.
Nat Chem Biol

Synergistic protection of nascent DNA at stalled forks by MSANTD4 and BRCA1/2-RAD51. [Abstract]

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).
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

LAP2α drives breast tumorigenesis by mitigating replication stress. [Abstract]

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
bioRxiv

2026 Mar 13.
bioRxiv

2025 Sep 21.

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.
bioRxiv

Replication competition drives the selective mtDNA inheritance in Drosophila ovary. [Abstract]

2025 May 3:2025.04.29.650984. PMID: 40568099
University of Zurich

2025 Feb 04.
bioRxiv

2024 August 31.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

2.9544 mL

14.7719 mL

29.5438 mL

5 mM

0.5909 mL

2.9544 mL

5.9088 mL

10 mM

0.2954 mL

1.4772 mL

2.9544 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, 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.

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: ≥ 2.5 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.

Protocol 2

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.

Protocol 3

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

Solubility: 2.5 mg/mL (7.39 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (282 KB)
SDS (393 KB)
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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]. 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]

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, 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

15 Cited Publications

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Aphidicolin

MCE Bioactive Compound Library

Natural Product Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Aphidicolin

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Alle HSV Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aphidicolin

MCE Bioactive Compound Library

Natural Product Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Aphidicolin

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Alle HSV Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aphidicolin Related Classifications

Art. -Nr.: HY-N6733