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PARP/EZH2-IN-1

Names

[ CAS No. ]:
2687273-52-3

[ Name ]:
PARP/EZH2-IN-1

Biological Activity

[Description]:

PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

PARP-1:6.87 nM (IC50)

EZH2:36.51 nM (IC50)

[References]

[1]. Wang C, et al. Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA. J Med Chem. 2021 Sep 9;64(17):12630-12650.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₃H₄₁FN₈O₅

[ Molecular Weight ]:
768.83

Related Compounds