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.
For research use only. We do not sell to patients.
- Formula: C39H43ClN8O4
- Molecular Weight:723.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PARP-1 28 nM (IC50) |
PARP2 414 nM (IC50) |
EZH2 74 nM (IC50) |
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.
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Cell Line:BT-549 cells
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Concentration:1.0, 1.5 and 2.0 μM
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Incubation Time:24 h
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Result:Inhibited the invasion of TNBC cells.
Suppressed cell migration in scratch-wound repair.
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Cell Line:BT-549 cells
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Concentration:1.0, 1.5 and 2.0 μM
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Incubation Time:24 h
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Result:Inhibited the invasion of TNBC cells.
Suppressed cell migration in scratch-wound repair.
Exhibited a stronger inhibitory effect on TNBC cells
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Cell Line:BT-549 cells
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Concentration:2.0 μM
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Incubation Time:48 h
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Result:Decreased the expression levels of PAR, H3K27me3, BRCA1 and RAD51 proteins.
Increased the expression level of γ-H2AX.
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Cell Line:TNBC cell
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Concentration:0.625, 1.25, 2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Suppressed TNBC cell viability in a manner dependent on ROS accumulation, as evidenced by the significant reversal of this effect upon co-treatment with the ROS scavenger NAC.
| Species | Dose | Route | C0 | AUC0-t | AUC0-∞ | T1/2 | Vd/F | CL/F | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 2 mg/kg | i.v. | 9.92 mg/L | 0.89 mg·h/L | 0.92 mg·h/L | 0.44 h | 1.36 L/h/kg | 2172 L/h/kg | 0.08 h |
Chemical Information
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Molecular Weight 723.26
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Formula C39H43ClN8O4
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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