Hycanthone 是 Lucanthone 的生物活性代谢产物，是一种抗血吸虫病药。它是一个噻吨酮类 DNA 嵌入剂，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。它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，KD为 10 nM。

Hycanthone is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Hycanthone at 20 mg/mL or more is progressively more detrimental to cell viability. Compared to that of controls, results show that increased concentrations of Hycanthone, ranging from 0.1 to 10 μg/mL, progressively decreases viral interferon yields as much as 73% [2].

Male worms treated with Hycanthone display signs of possible partial recovery from the initial low levels of incorporation. After treatment with Hycanthone, the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease. Immature worms are totally unaffected by Hycanthone at all times tested. In the first four days after treatment, incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50%. 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 [1].

3105-97-3

C20H24N2O2S

356.48

海恩酮;Etrenol(mesylate);Win 249-33

DMSO:18 mg/mL (50.49 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years