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. 2020 Dec 3;3(1):vdaa165. doi: 10.1093/noajnl/vdaa165

Figure 1.

Figure 1.

Activity of ST-401 and its analogues at the colchicine site of tubulin, and MT assembly and dynamics. (A) Diagram of MTA binding sites on tubulin. (B) ST-401 and its analogues are based on an N-ethyl-carbazole moiety (green) linked via a ketone (ST-34, ST-360, red) or a secondary alcohol (ST-377, ST-401, purple) to either a quinoline (ST-360, ST-401, blue) or a methyl-naphthalene residue (ST-34, ST-377, orange). (C) ST-compounds (5 μM) compete for [3H]colchicine-binding to tubulin. Results are mean ± SD from n = 3 experiments. Dotted line shows vehicle control (5% DMSO). (D) ST-compounds inhibit tubulin assembly measured by turbidity development of tubulin solutions. Representative IC50 values from 3 experiments with comparable results. (E) ST-401 and ST-360 inhibit tubulin assembly measured in a pelleting assay. Results are mean ± SEM from 3 to 5 experiments. (F) ST-401 and nocodazole (NOC) reversibly inhibit MT assembly rates in HCT116 cells when comparing measures before (I), during (II), and after (III) treatment. N = 10–15 individual cells.