2. Cell Cycle/DNA Damage Epigenetics GPCR/G Protein Stem Cell/Wnt NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. PARP CDK Protease Activated Receptor (PAR) Wnt β-catenin Reactive Oxygen Species (ROS) DNA/RNA Synthesis
  4. 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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PC8

PC8 Chemical Structure

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PC8 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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[1].

IC50 & Target[1]

CDK6

0.197 μM (IC50)

PARP1

0.126 μM (IC50)

In Vitro

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.

PC8 Related Antibodies

Western Blot Analysis[1]

Cell Line: BT-549 TNBC cells
Concentration: 0.5-1.5 μM
Incubation Time: 48 h
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.
Molecular Weight

578.50

Formula

C28H32BrN7O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PC8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PC8PC 8PC-8PARPCDKProtease Activated Receptor (PAR)Wntβ-cateninReactive Oxygen Species (ROS)DNA/RNA Synthesispoly ADP ribose polymerase Cyclin dependent kinaseThrombin receptorsBeta cateninMDA-MB-468ROSCDK6mitochondrial dysfunctionBT-549Wnt signaling pathwayMDA-MB-231triple-negative breast cancerPARP1TNBC cellsInhibitorinhibitorinhibit

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