PMV6-PEG4-BI2536 is a dual-functional compound targeting both p53-Y220C and PLK1. It consists of a high-affinity binder for the p53-Y220C mutant (Kd≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50= 0.83 nM). This compound induces G2/M arrest and apoptosis in TP53Y220C cells through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 is applicable for researching TP53 mutant cancers.

PLK1:0.83 nM