Aphidicolin阿非迪霉素,38966-21-1

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Aphidicolin

CAS No. : 38966-21-1

MCE 国际站：Aphidicolin

产品活性：Aphidicolin 是 DNA 聚合酶 α 和 δ 抑制剂，通过干扰 DNA 聚合酶的活性来阻止细胞有丝分裂。Aphidicolin 是一种来源于 Cephalosporium aphidicola 的抗生素, 能够抑制细胞脱氧核糖核酸合成和单纯疱疹病毒生长。Aphidicolin 具有抗正痘病毒活性，能够增强阿拉伯糖基核苷对细胞凋亡 (apoptosis) 的诱导作用。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection  |  Apoptosis

作用靶点：DNA/RNA Synthesis  |  HSV  |  Apoptosis  |  Antibiotic  |  Orthopoxvirus

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.

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%.

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