Tubulin polymerization/P-gp-IN-1

Tubulin polymerization/P-gp-IN-1 (Compound 6h) not only confers high potency in sensitive cells such as HeLa cells (IC₅₀ = 6.69 μM), CaSki cells (IC₅₀ = 7.84 μM), and SiHa cells (IC₅₀ = 16.68 μM), but also maintains nearly equivalent efficacy against the drug-resistant HeLa/DDP cell line (IC₅₀ = 7.21 μM), and shows no significant cytotoxicity against human normal cervical cells (IC₅₀ = 51.95 μM)^[1].
Tubulin polymerization/P-gp-IN-1 (4-16 μM, 24 h) decreases the levels of polymerized α- and β-tubulin, while the levels of depolymerized tubulin increase, with effects similar to colchicine (COL) but opposite to paclitaxel (PTX), and causes microtubule network contraction (especially 8 μM and 16 μM), and the cell morphology changed from spindle-shaped to round, with microtubules remaining only in the perinuclear region in HeLa and HeLa/ DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (4-16 μM, 24 h) not only induces G₂/M cell cycle arrest but also effectively triggers apoptosis and significantly suppresses in vitro migration in a concentration-dependent manner in both HeLa and HeLa/DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (0.25-1 μM, 48 h) can effectively reverse Cisplatin resistance in HeLa/DDP cells^[1].
Tubulin polymerization/P-gp-IN-1 (0.25-1 μM, 12 h) not only concentration-dependently inhibits P-gp-mediated efflux but also maintains unchanged P-gp protein levels at 1 μM in HeLa/DDP cells, and it significantly stabilizes P-gp under elevated temperatures of 61 °C^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.