2. Cell Cycle/DNA Damage Anti-infection Apoptosis
  3. DNA/RNA Synthesis HSV Apoptosis Antibiotic Orthopoxvirus
  4. Aphidicolin

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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Aphidicolin Chemical Structure

Aphidicolin Chemical Structure

CAS No. : 38966-21-1

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1 mg USD 150 In-stock
5 mg USD 580 In-stock
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50 mg USD 3620 In-stock
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Based on 5 publication(s) in Google Scholar

Other Forms of Aphidicolin:

Aphidicolin Related Antibodies

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  • Biological Activity

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Description

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[1][2][3].

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]
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]
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]
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.

Aphidicolin Related Antibodies

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.
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

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
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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 5 mg/mL (14.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (14.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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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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: 99.84%

SDS (393 KB)

COA (250 KB) RP-HPLC (1088 KB)

Handling Instructions (2659 KB)
References

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
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Aphidicolin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Aphidicolin38966-21-1DNA/RNA SynthesisHSVApoptosisAntibioticOrthopoxvirusHerpes simplex viruspromyelocytic leukemia cellcellular deoxyribonucleic acid synthesisherpes simplex virusDNA polymerasemitotic cell divisionanti-orthopoxvirusarabinosyl nucleosidesneuroblastoma cellscell killingACTHPOMCpituitaryCushing’s diseasepituitary corticotroph tumor cellsInhibitorinhibitorinhibit

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