产品
编 号：F122541
分子式：C20H13BrN2O3S2
分子量：473.36
分子式：C20H13BrN2O3S2
分子量：473.36
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CAS No: 1332879-52-3
产品详情
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.
体外研究：
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.
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.
体外研究：
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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