PARP1-IN-55
PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3109617-69-5
- Formula: C25H35NO5
- Molecular Weight:429.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
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Biological Activity
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PARP1 0.019 μM (IC50) |
PARP1-IN-55 (compound 3f) (48 h) exhibits potent antiproliferative activity and high selectivity against MCF-7 cells, while it shows minimal cytotoxicity against L-02 cells (IC50 > 100 μM) with a selectivity index (SI) exceeding 27[1].
PARP1-IN-55 (1-10 μM; 48 h) inhibits the expression of intracellular PARP1 in MCF-7 cells in a dose-dependent manner[1].
PARP1-IN-55 (1-10 μM; 14 days) inhibits the colony formation of MCF-7 cells in a concentration-dependent manner, and completely suppresses the colony formation at 10 μM with little effect on L-02 cells[1].
PARP1-IN-55 (1-10 μM; 24 h, 48 h) inhibits the migration and invasion of MCF-7 cells in a dose-dependent manner, and significantly downregulates the expression of COL1 in MCF-7 cells at 10 μM[1].
PARP1-IN-55 (3-10 μM; 48 h) induces apoptosis in MCF-7 cells, which causes early apoptosis at 3 μM and mainly late apoptosis at 5 μM and 10 μM, with minimal apoptotic effect on L-02 cells[1].
PARP1-IN-55 (1-10 μM) induces a significant dose-dependent increase in intracellular ROS levels, reduces mitochondrial membrane potential (MMP), and disrupts cell membrane integrity as well as induces extensive cell death in MCF-7 cells, while it causes almost no effect on L-02 cells. [1].
PARP1-IN-55 (1-10 μM; 24 h) increases the level of γH2AX protein in MCF-7 cells, inhibits the PARP1-mediated DNA damage repair pathway, and causes the accumulation of DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Induced a significant concentration-dependent increase in the number of nuclear γH2AX fluorescence foci, indicating accumulation of DNA double-strand breaks.
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Cell Line:MCF-7 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:24 h, 48 h
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Result:Inhibits the invasion of MCF-7 cells in a dose-dependent manner, with the inhibitory effect at 10 μM significantly stronger than that of isoalantolactone.
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Cell Line:MCF-7 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:24 h, 48 h
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Result:Inhibits the migration of MCF-7 cells in a dose-dependent manner.
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Cell Line:MCF-7, L-02 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:14 days
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Result:Inhibits colony formation of MCF-7 cells in a concentration-dependent manner, completely suppressing colony formation at 10 μM; little effect on L-02 cells.
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Cell Line:MCF-7, L-02 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Disrupts the cell membrane integrity of MCF-7 cells, inducing extensive cell death; no effect on the viability of L-02 cells.
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Cell Line:MCF-7, L-02 cells
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Concentration:3 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Induces early apoptosis at 3 μM and mainly late apoptosis at 5 μM/10 μM in MCF-7 cells; minimal apoptotic effect on L-02 cells.
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Cell Line:MCF-7 cells
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Concentration:1 μM, 3 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Dose-dependently decreased nuclear PARP1 expression and increased γH2AX expression.
Significantly downregulated COL1 expression at 10 μM.
Chemical Information
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CAS No. 3109617-69-5
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Molecular Weight 429.55
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Formula C25H35NO5
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SMILES
O=C1C(CNCC2=CC(OC)=C(OC)C(OC)=C2)[C@@]3([H])C[C@@]4([H])C(CCC[C@]4(C)C[C@@]3([H])O1)=C
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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)
- PARP1-IN-55
- 3109617-69-5
- PARP
- DNA/RNA Synthesis
- Reactive Oxygen Species (ROS)
- Apoptosis
- PARP1 inhibitor
- apoptosis
- elevate ROS
- decrease mitochondrial membrane potential
- inhibit migration and invasion
- inhibit colony formation
- suppress DNA damage repair
- breast cancer
- MCF-7 cells
- AGS cells
- SW620 cells
- SU-DHL-10 cells
- L-02 cells
- Inhibitor
- inhibitor
- inhibit