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。

Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a K D of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.

Solid

Topoisomerase I Topoisomerase II

Hycanthone has an IC50 of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA.
Hycanthone (0.05-100 μM; 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for refer

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Mamta D Naidu, et al. Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding. PLoS One. 2011;6(9):e23679.
[2]. Pica Mattoccia L, et al. Effect of hycanthone administered in vivo upon the incorporation of radioactive precursors into macromolecules of Schistosoma mansoni. Mol Biochem Parasitol. 1983 Jun;8(2):99-107.

In Vitro: DMSO : 12.5 mg/mL (35.07 mM; Need ultrasonic)配制储备液