Aphidicolin

Name: Aphidicolin
Brand: MedChemExpress
SKU: HY-N6733
Rating: 5.0 (15 reviews)

Cat. No.: HY-N6733 Purity: 99.93%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 38966-21-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Aphidicolin:

Aphidicolin (Standard) Get quote

15 Publications Citing Use of MCE Aphidicolin

Cell Proliferation/Viability Assay

RT-PCR

: 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).

: 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.

: 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).

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DNA Polymerase

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]

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.

Molecular Weight

338.48

Formula

C₂₀H₃₄O₄

CAS No.

38966-21-1

Appearance

Solid

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

Initial Source

Microorganisms

Cephalosporium aphidicola

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (250 KB) RP-HPLC (281 KB)

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

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 Related Classifications

Inflammation/Immunology Infection

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Aphidicolin

Customer Review

Other Forms of Aphidicolin:

15 Publications Citing Use of MCE Aphidicolin

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Aphidicolin

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Other Forms of Aphidicolin:

Aphidicolin Related Antibodies

15 Publications Citing Use of MCE Aphidicolin

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Aphidicolin Related Antibodies

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Complete Stock Solution Preparation Table

Aphidicolin Related Classifications

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