PARP1-IN-49
PARP1-IN-49 is a selective PARP1 inhibitor with an IC50 of 23.56 nM and a Kd of 17.78 nM. PARP1-IN-49 shows a selectivity for PARP1 over PARP2. PARP1-IN-49 leads to the induction of DNA damage, cell cycle arrest, and apoptosis. PARP1-IN-49 also increases intracellular ROS levels and inhibits cell migration. PARP1-IN-49 can be used for the research of breast cancer and ovarian cancer.
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- Fòrmula: C15H11FN2O3
- Peso molecular:286.26
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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PARP1 23.56 nM (IC50) |
PARP1 17.78 nM (Kd) |
PARP2 285.39 nM (IC50) |
PARP1-IN-49 (compound 9a) (0.5-2 μM; 48 h) inhibits MDA-MB-231 cell proliferation and migration[1].
PARP1-IN-49 (0.5-2 μM; 48 h) increases apoptosis-related protein expression and decreases Bcl-2 levels in MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-2 μM; 48 h) induces DNA damage and double-strand breaks MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-2 μM; 48 h) increases apoptosis and causes S phase cell cycle arrest MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-4 μM; 48 h) induces apoptosis via ROS generation and altered mitochondrial membrane potential MDA-MB-231 cells[1].
PARP1-IN-49 (2 μM; 48 h) enhances PARP1 thermal stability, indicating direct interaction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:Inhibited cell proliferation and migration in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner, increasing the expression of apoptosis-related proteins, such as Cleaved PARP, Cleaved caspase3 and Bax, and decreasing Bcl-2 protein levels.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:Induced DNA damage and the accumulation of double-strand breaks, as indicated by increased γH2AX and comet tail length.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:The proportion of cells in the S phase increased from 20.09% to 47.56%, while the proportion of cells in the G2/M phase decreased from 19.11% to 6.58%.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:The proportion of cells undergoing early and late apoptosis increased from 0.49% to 53.8%.
| Species | Dose | Route | Note | Tmax | Cmax | AUC0-t | T1/2 | MRT |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.p. | 文献审核 | 0.39 h | 6993.33 ng/mL | 11115.57 ng·h/mL | 1.5 h | 1.13 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 cells (1 × 107 cells) were subcutaneously inoculated into the right flank of BALB/c nude mice (4-week-old)[1]
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Dosage:20 mg/kg, 40 mg/kg
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Administration:Intraperitoneal; 22 days
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Result:Tumor growth was significantly inhibited.
Chemical Information
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Peso molecular 286.26
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Fòrmula C15H11FN2O3
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SMILES
O=C(NC)C1=CC(C2=CC=C(OC(N3)=O)C3=C2)=CC(F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP1-IN-49 Related Classifications
HY-179406 Related Classifications
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