MI-181

MI-181 may be used to evaluate its anti-cancer properties in various cancer cell lines, demonstrating activity against a broad spectrum of cancers, including melanomas harboring specific mutations like BRAFV600E.

MI-181, a potent small synthetic microtubule-targeting anticancer agent, acts as a mitotic inhibitor, arresting cancer cells during the M-phase of the cell cycle. It inhibits microtubule polymerization, arrests cells in mitosis, activates the spindle assembly checkpoint, and/or triggers apoptotic cell death.


MI-181 serves as a microtubule destabilization agent that targets β-tubulin near the colchicine-binding site and causes microtubule depolymerization, activates the spindle assembly checkpoint (SAC), arrests cells in mitosis (76.6%, IC50 = 23.6 nM post 20h treatment of HeLa), and induces apoptotic death in cancer cultures (HeLa/M233/NCI-H460/U2OS/CCRF-CEM viability IC50 post 72h = 30//30/36/60/100 nM). MI-181 is also a potent modulator of cilia length and biogenesis (length post 24h with/without 100 nM MI-181 = 6.09/3.52 μm (serum withdrawal) or 4.75/2.97 μm (with serum); hTERT RPE-1 cells), while microtubule destabilizers (10 μM colchicine, 116 nM nocodazole) and stabilizer (100 nM paclitaxel) causes decreased cilia length.