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AK306(AK 306;AK-306) is a small molecule clathrin heavy chain (CLTC/CHC) binding compound that induces arrest and apoptosis of the HCT116 colon cancer cell line with EC50 of 50 nM; demonstrates broad spectrum activity against of cancer cell lines with total growth inhibition values ranging from ~25 nM to 25 uM; disrupts Aurora A localization, leading to the formation of multiple foci, induces a p53-dependent cell death, and centrosome disruption.
Pitstop 1 (Pitstop-1;Pitstop1) is a potent, selective inhibitor of clathrin-independent endocytosis with IC50 of 18 uM (inhibition of clathrin TD-amphiphysin B/C complex formation); inhibits endocytic recycling of synaptic vesicles in neurons and in situ.
Pitstop 2 (Pitstop-2;Pitstop2) is a small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis; inhibits endocytosis of transferrin receptor, a CDE cargo protein, but not affect endocytosis of shiga toxin; traps HeLa cells in metaphase through loss of mitotic spindle integrity and activation of the spindle assembly checkpoint, a useful tool for investigating clathrin spindle dynamics.
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