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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Hycanthone
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
3105-97-3
- 规格：
5mg/10mg
| 规格： | 5mg | 产品价格： | ￥302.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥490.0 |
| 基本信息 | |
| CAS | No.3105-97-3 |
| 中文名称 | 海恩酮 |
| 英文名称 | Hycanthone |
| 别名 | Etrenol(mesylate);Win 249-33 |
| 分子式 | C20H24N2O2S |
| 分子量 | 356.48 |
| 溶解性 | Soluble in DMSO ≥1mg/mL(Need ultrasonic) |
| 纯度 | ≥95% |
| 外观(性状) | Yellow to orange Soild |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00083383 |
| InChIKey | MFZWMTSUNYWVBU-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H24N2O2S/c1-3-22(4-2)12-11-21-16-10-9-14(13-23)20-18(16)19(24)15-7-5-6-8-17(15)25-20/h5-10，21，23H，3-4，11-13H2，1-2H3 |
| PubChem CID | 3634 |
| 靶点 | DNA/RNA Synthesis;Topoisomerase;Parasite |
| 通路 | Cell Cycle;DNA Damage/DNA Repair;Anti-infection |
| 背景说明 | Hycanthone是一种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)。Hycanthone具有抗血吸虫活性。 |
| 生物活性 | 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 KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.[1-3] |
| In Vitro | Hycanthone has an IC50 of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA[1]. Hycanthone (0.05-100 μM; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO[1]. 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[3]. |
| 细胞实验 | 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[2]. |
| 细胞实验 | Appropriate quantities of Hycanthone (1 to 100 μg) in 10 mL maintenance medium are added to plastic flasks (75 cm2) containing approximately 3×107 LLC-MK2 cells in monolayer， which are then incubated at 35°C for 24 h. Maintenance medium is decanted， and 2 mL influenza virus is added onto cell monolayers and incubated at 35°C for 2 h. The multiplicity of infection is approximately 1.0. Inoculum is removed and 10 mL maintenance medium is added to each flask， which is then incubated at 35°C for 24 h. Supernatant fluid is decanted， centrifuged at 100，000 g for 1 h， dialyzed against HCI-KCI buffer (pH 2.0) at 4°C for 24 h， and then dialyzed against two changes of phosphate-buffered saline (pH 7.1) at 4°C for 24 h. Fluids are passed through filters to obtain sterile preparations. Samples are stored at -80°C until assayed for interferon activity[2]. |
| 动物实验 | Female outbred Swiss albino mice used as definitive hosts weigh 18 to 20 g at the time of infection. Hycanthone is administered at 0.01 mL/g body weight intramuscularly by splitting the dose into the two hind legs， so that each mouse receives 80 mg/kg body weight of the free base. Treatments are usually performed during the 8th week after infection[1]. |
| 数据来源文献 | [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. [3]. Hahon N， et al. Action of antischistosomal drugs， hycanthone and its analog 1A-4 N-oxide， on viral interferon induction. J Toxicol Environ Health. 1980 Jul;6(4):705-12. |
| 单位 | 瓶 |
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