计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 的生物活性代谢产物，具有抗血吸虫病活性分子。
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 and has anti-schistosomal agent
In Vitro
Hycanthone has an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
Appropriate quantities of Hycanthone (1 to 100 μg) in 10 mL maintenance medium are added to plastic flasks (75 cm 2 ) containing approximately 3×10 7 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Topoisomerase I Topoisomerase II
规格
别名
氢化松
规格或纯度
10mM in DMSO
英文名称
Hycanthone
生化机理
Hycanthone 是一种硫代蒽酮 DNA 中间体，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。Hycanthone 可抑制核酸的生物合成，并通过直接蛋白结合抑制 apurinic endonuclease-1 (APE1)，其 K D 值为 10 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
EC号
221-463-7
分子类型
小分子
Isomeric SMILES
CCN(CC)CCNC1=C2C(=C(C=C1)CO)SC3=CC=CC=C3C2=O
PubChem CID
分子量
356.48
技术文档
高级数据
关联靶点（人）
CYP1A2
Tchem
细胞色素 P450 1A2(Cytochrome P450 1A2)
(1 活性数据)
APEX1
Tchem
DNA（脱嘌呤或脱嘧啶位点）裂解酶(DNA-(apurinic or apyrimidinic site) lyase)
(2 活性数据)
安全和危险性（GHS）
信号词
Danger
危险声明
H302: 吞食有害
H312: 皮肤接触有害
H332: 吸入有害
H350: 可能导致癌症
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P302+P352: 如皮肤沾染：用水充分清洗。
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P271: 仅在室外或通风良好的地方使用。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。
P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。
P330: 漱口
P203: 使用前，获取、阅读并遵守所有安全说明。
P301+P317: 如果被吞咽：请寻求医疗帮助。
P318: 如果暴露或担心，请就医。
P317: 寻求紧急医疗救助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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