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PMV6-PEG4-BI2536

PMV6-PEG4-BI2536 is a p53-Y220C-PLK1 dual-functional compound, composed of a high-affinity p53-Y220C mutant binder (Kd ≈ 2.5 nM) and a potent PLK1 kinase inhibitor (IC50 = 0.83 nM) . PMV6-PEG4-BI2536 triggers TP53Y220C cell G2/M arrest and apoptosis through PLK1 mislocalization and kinase inhibition, independent of p53 transcriptional reactivation. PMV6-PEG4-BI2536 can be used for the study of TP53 mutant cancers[1].

Product Specifications

UNSPSC

12352005

Target

MDM-2/p53; Polo-like Kinase (PLK)

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Field of Research

Cancer

Smiles

O=C(NCCOCCOCCOCCOCCC(N1CCC(NC2=CC=CC3=C2C=C(C#CCNC4=CC=C(S(=O)(C)=O)C=C4OC)N3CC(F)(F)F)CC1)=O)C5=CC=C(NC(N=C6N(C7CCCC7)[C@@H]8CC)=NC=C6N(C)C8=O)C(OC)=C5

Molecular Formula

C59H75F3N10O11S

Molecular Weight

1189.35

References & Citations

[1]Sadagopan A, et al. Mutant p53 protein accumulation is selectively targetable by proximity-inducing drugs. Nat Chem Biol. 2025 Nov 3.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PLK1

Curated Selection

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