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Clathrin-IN-1

CAS No. : 1332879-52-3

MCE 站：Clathrin-IN-1

产品活性：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。

研究领域：Anti-infection

作用靶点：HIV

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.
Clathrin-IN-1 (Pitstops 2) potently and specifically reduced HIV-1 infectivity by >90% in HeLa cells.
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.

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