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].

PARP1/EZH2-IN-1 (compound PE32) (72 h) has IC₅₀ of 2.85 μM, 1.83 μM and 1.46 μM for MDA-MB-231, MDA-MB-468 and BT-549, respectively^[1].
PARP1/EZH2-IN-1 (1.0-2.0 μM, 24 h) demonstrates stronger inhibitory effects on BT-549 cells invasion, migration, and scratch-wound repair^[1].
PARP1/EZH2-IN-1 (0.5-2.0 μM, 48 h) inhibits the proliferation and growth of MDA-MB-231, BT-549 cells^[1].
PARP1/EZH2-IN-1 (2.0 μM, 48 h) leads to intensified DNA damage and disrupts the homologous recombination repair pathway in BT-549 cells^[1].
PARP1/EZH2-IN-1 (1.5 μM, 48 h) causes the death of BT-549 cells by inducing apoptosis and pyroptosis of the cells^[1].
PARP1/EZH2-IN-1 (0.625-10 μM, 48 h) exerts the antitumor effect primarily through triggering a ROS burst in BT-549 cells^[1].
PARP1/EZH2-IN-1 enriches tumor-related death pathways, including transcriptional misregulation in cancer, ECM-receptor interaction, and TNF signaling, activates key inflammatory pathways, such as IL-17 and NF-κB, and induces tumor cell pyroptosis through activating these critical inflammatory signaling cascades^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

723.26

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• [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.  [Content Brief]