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Hycanthone
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Hycanthone
CAS No. : 3105-97-3
MCE 站:Hycanthone
产品活性:Hycanthone 是噻吨酮类的 DNA 嵌入剂 (DNA intercalator),可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。Hycanthone 通过直接蛋白质结合来抑制核酸生物合成并抑制嘌呤内切核酸酶1 (APE1),KD 为 10 nM。Hycanthone 是 Lucanthone (HY-B2098) 的生物活性代谢产物,具有抗血吸虫病药物。
研究领域:Cell Cycle/DNA Damage | Anti-infection
作用靶点:DNA/RNA Synthesis | Topoisomerase | Parasite
In Vitro: Hycanthone has an IC50 of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA.
Hycanthone (0.05-100 ?M; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO.
Hycanthone at 20 mg/mL or more is progressively more detrimental to cell viability. Results reveal that increased concentrations of Hycanthone, ranging from 0.1 to 10 μg/mL, progressively reduces viral interferon yields as much as 73% compare to that of controls.
In Vivo: Results show that the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease after treatment with Hycanthone. Immature worms are totally unaffected by Hycanthone at all times tested. Male worms treated with Hycanthone show signs of a possible partial recovery from the initial low levels of incorporation. The incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50% in the first four days after treatment. Results show that, 7 days after Hycanthone treatment, both ribosomal RNA species are reduced by at least 80% with respect to untreated worms, with some indication of a possible accumulation of heavier precursor molecules.
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