PARP1/EZH2-IN-1

PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells) . PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase; Necroptosis; PARP; Pyroptosis; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

CCC1=CC(N=CC(CN2CCN(C3=NC=C(C4=CC(N(C(CCl)=O)CC)=CC(C(NCC5=C(C)C=C(C)NC5=O)=O)=C4)C=C3)CC2)=C6)=C6NC1=O

Molecular Formula

C39H43ClN8O4

Molecular Weight

723.26

References & Citations

[1]Fan H, et al, . Discovery of selective PARP1/EZH2 inhibitor inducing PANoptosis in triple-negative breast cancer. Eur J Med Chem. 2026 Jan 15;302 (Pt 2) :118287.