Hycanthone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Hycanthone 是一种强效抗血吸虫药。 Hycanthone 是一种 DNA 嵌入剂，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。

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).(In Vitro):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% . (In Vivo):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 .

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.

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.

Win 249-33 | Etrenol(mesylate)

Cell Cycle/DNA Damage

DNA/RNA Synthesis

Drug-Linker Conjugates for ADC| Microtubule/Tubulin

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3105-97-3

356.48

C20H24N2O2S

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (35.07 mM)

CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12

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(-20℃)

With Ice Pack

≥ 2 years