321695-37-8

Poloxin-2 is a potent Plk1 PBD inhibitor. It acts by inducing mitotic arrest and apoptosis in cultured human tumor cells at low micromolar concentrations.

Poloxin-2 is a small molecule Plk1 PBD inhibitor that can effectively induce cell mitotic arrest with an EC50 of approximately 15 μM in HeLa cells. Poloxin-2HT was developed by conjugating a hydrophobic tag (HT) to Poloxin-2, a new application of inhibitors targeting protein-protein interactions. Poloxin-2HT significantly enhanced the effects on cell viability and apoptosis by selectively degrading Plk1 protein, and its effect was stronger than that of untagged Poloxin-2. These data validate hydrophobic tags as a new strategy for targeting and disrupting disease-associated proteins.

[1] Optimized Plk1 PBD inhibitors based on Poloxin induce mitotic arrest and apoptosis in tumor cells