YCH3971
YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors.
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- Fòrmula: C23H25N5O
- Peso molecular:387.48
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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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PARP-1 7.52 nM (IC50) |
PARP-1 67.75 nM (EC50) |
YCH3971 (0.01-10000 nM, 7 days) potently inhibits the proliferation of BRCA1-deficient MDA-MB-436 cells, with an IC50 of 2.10 nM[1].
YCH3971 (0.01-10000 nM, 7 days) inhibits the proliferation of BRCA2-deficient V-C8 cells with an IC50 of 69.61 nM, while it exhibits only extremely weak activity against BRCA2-proficient V79 cells[1].
YCH3971 (0.01-10000 nM, 7 days) inhibits the proliferation of BRCA1-mutant UWB1.289 ovarian cancer cells with an IC50 of 112.86 nM, whereas it shows almost no activity against UWB1.289 + BRCA1 cells with restored BRCA1 expression[1].
YCH3971 (0.01-1 μM; 48 h) induces dose-dependent DNA damage in MDA-MB-436 cells[1].
YCH3971 (0.01-1 μM; 3 days) induces dose-dependent G2/M phase arrest in MDA-MB-436 cells[1].
YCH3971 (0.01-1 μM; 4 days) induces dose-dependent caspase-mediated apoptosis in MDA-MB-436 cells[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-436 cells
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Concentration:0, 0.01, 0.1, 1 μM
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Incubation Time:48 h
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Result:Induced dose-dependent DNA damage.
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Cell Line:MDA-MB-436 cells
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Concentration:0, 0.01, 0.1, 1 μM
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Incubation Time:3 days
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Result:Led to a dose-dependent accumulation of cells in the G2/M phase.
At concentrations ≥0.1 μM, caused a statistically significant increase in G2/M phase cells.
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Cell Line:MDA-MB-436 cells
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Concentration:0, 0.01, 0.1, 1 μM
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Incubation Time:4 days
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Result:Led to a dose-dependent increase in Annexin V+/PI+ apoptotic cells.
At 1 μM, induced a slightly higher level of apoptosis.
Confirmed dose-dependent cleavage of caspases-3, -7, and -8 via western blotting.
At 1 μM, induced slightly stronger caspase activation.
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Cell Line:MDA-MB-436 cells
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Concentration:0, 0.01, 0.1, 1 μM
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Incubation Time:48 h
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Result:Activated DNA damage response markers, including phosphorylated CHK1 (p-CHK1), phosphorylated RPA32 (p-RPA32), and γH2AX.
Chemical Information
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Peso molecular 387.48
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Fòrmula C23H25N5O
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SMILES
CC1=C(N2CCN(CC3=CN4C(C=C(C5CC5)C(N4)=O)=C3)CC2)C=CC(C#N)=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)
YCH3971 Related Classifications
HY-181664 Related Classifications
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