PC8
PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.
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- Fòrmula: C28H32BrN7O2
- Peso molecular:578.50
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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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CDK6 0.197 μM (IC50) |
PARP1 0.126 μM (IC50) |
PC8 potently and selectively inhibits purified PARP1 with an IC50 of 0.126 μM, whereas it shows weak inhibitory activity against PARP2 (IC50 = 0.824 μM)[1].
PC8 potently inhibits purified CDK6 with an IC50 of 0.197 μM, and exhibits only limited activity against most other members of the CDK family[1].
PC8 (72 h) potently inhibits the proliferation of three triple-negative breast cancer (TNBC) cell lines, namely MDA-MB-231 (IC50 = 1.14 μM), MDA-MB-468 (IC50 = 1.25 μM), and BT-549[1].
PC8 (0.5-1.5 μM; 48 h) inhibits the downstream pathway of PARP1 and induces DNA damage in BT-549 triple-negative breast cancer (TNBC) cells[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 TNBC cells
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Concentration:0.5-1.5 μM
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Incubation Time:48 h
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Result:Did not alter PARP1 expression, but reduced PAR expression.
Reduced CDK6 expression slightly and RB1 expression markedly.
Reduced RAD51 and BRCA1 levels, and increased γ-H2AX levels.
Upregulated E-cadherin expression and downregulated N-cadherin and Vimentin expression.
Reduced expression of β-catenin, Axin2, P-GSK3β, and Wnt3a.
Chemical Information
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Peso molecular 578.50
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Fòrmula C28H32BrN7O2
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SMILES
O=C1C(Br)=C(C)C2=CN=C(N[C@@H]3CN(CC4=CC(N5)=C(N=C4)C=C(CC)C5=O)CC3)N=C2N1C6CCCC6
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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)
PC8 Related Classifications
HY-181999 Related Classifications
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