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  2. HIV
  3. Clathrin-IN-1

Clathrin-IN-1 

目录号: HY-102068
产品使用指南

Clathrin-IN-1 是一种选择性网格蛋白介导的内吞 (CME) 抑制剂。Clathrin-IN-1 选择性抑制两性蛋白与网格蛋白氨基末端结构域的结合,IC50 值为 12 μM。Clathrin-IN-1 干扰受体介导的内吞作用,HIV 的进入和突触小泡的回收。

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Clathrin-IN-1 Chemical Structure

Clathrin-IN-1 Chemical Structure

CAS No. : 1332879-52-3

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  • 生物活性

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  • 参考文献

生物活性

Clathrin-IN-1 is a selective clathrin-mediated endocytosis (CME) inhibitor. Clathrin-IN-1 selectively inhibits amphiphysin association of clathrin terminal domain (TD) with an IC50 value of 12 μM. Clathrin-IN-1 acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling[1].

体外研究
(In Vitro)

Preincubation of HeLa cells with Clathrin-IN-1 (Pitstops 2) leads to a dose-dependent inhibition of Tf uptake with an IC50 value (12-5 μM). Application of 30 μM Clathrin-IN-1 completely blocked Tf endocytosis. Clathrin-IN-1-induced block of Tf endocytosis in HeLa cells was completely reversed within 1-3 hr of drug washout. In U2OS cells, the IC50 for Tf uptake is 9.7 μM. Pitstop 2 also causes a potent inhibition of EGF uptake[1].
Clathrin-IN-1 (Pitstops 2) potently and specifically reduced HIV-1 infectivity by >90% in HeLa cells[1].
Pitstop-induced inhibition of clathrin TD function acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling. Endocytosis inhibition is caused by a dramatic increase in the lifetimes of clathrin coat components, including FCHo, clathrin, and dynamin, suggesting that the clathrin TD regulates coated pit dynamics[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

473.36

Formula

C20H13BrN2O3S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
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HY-102068
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