Ansamitocin P-3 (Antibiotic C 15003P3) exhibits potent anti-proliferative activity against MCF-7, HeLa, EMT-6/AR1, and MDA-MB-231 cell lines, with half-maximal inhibitory concentrations (IC50) of approximately 20±3, 50±0.5, 140±17, and 150±1.1 pM, respectively. It binds to tubulin with a dissociation constant (Kd) of about 1.3±0.7 μM, leading to tubulin's conformational changes. This compound not only significantly inhibits cell proliferation in a concentration-dependent manner but also stalls MCF-7 cell cycle progression in the G2/M phase as shown by flow cytometric analysis of propidium iodide-stained cells, with an increased percentage of cells in G2/M phase upon treatment with 50 and 100 pM Ansamitocin P3[2].
体外研究
Ansamitocin P-3 (Antibiotic C 15003P3) exhibits potent anti-proliferative activity against MCF-7, HeLa, EMT-6/AR1, and MDA-MB-231 cell lines, with half-maximal inhibitory concentrations (IC50) of approximately 20±3, 50±0.5, 140±17, and 150±1.1 pM, respectively. It binds to tubulin with a dissociation constant (Kd) of about 1.3±0.7 μM, leading to tubulin's conformational changes. This compound not only significantly inhibits cell proliferation in a concentration-dependent manner but also stalls MCF-7 cell cycle progression in the G2/M phase as shown by flow cytometric analysis of propidium iodide-stained cells, with an increased percentage of cells in G2/M phase upon treatment with 50 and 100 pM Ansamitocin P3[2].
Ansamitocin P-3/安丝菌素P 3 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Trypanosoma brucei
5 nM
4 h
To study the effect of Ansamitocin P-3 on KKT4 localization, results showed that after Ansamitocin P-3 treatment, KKT4 localized solely at kinetochores
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