Aphidicolin

SKU: orb2901626

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.

Key Properties

• CAS Number: 38966-21-1
• MW: 338.48
• Purity: >98% (HPLC)
• Formula: C₂₀H₃₄O₄
• SMILES: [H][C@]12C[C@]3([H])C[C@]1(CC[C@]3(O)CO)[C@@]1(C)CC[C@@H](O)[C@@](C)(CO)[C@]1([H])CC2
• Solubility: In Vitro: DMSO : 50 mg/mL (147.72 mM)

Bioactivity

• 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%. Animal model: M5076 sarcoma s. c. model or B16 melanoma i.p. model in murine. Dosage: 60 mg/kg, 100 mg/kg, 300 mg/kg. Administration: Intraperitoneal injection; once every 3 h; 9 days. Result: Inhibited tumor growth significantly.
  Read more...
• 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. Aphidicolin (0.4 μg/mL; 3 d) arrests cell cycle at G2 phase. 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. 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.Aphidicolin (10 μM; 0-6 h) inhibits Varicella-zoster virus (VZV) with EC50s of 0.5-0.6 μM, with low cytotoxicity. Cell Cytotoxicity Assay Cell line: NB cell lines: UKF-NB-1/2/3 and IMR-32. Concentration: 0.5 μM, 5 μM 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 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. 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only