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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)，K_D 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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