2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. PARP DNA/RNA Synthesis Reactive Oxygen Species (ROS) Apoptosis
  4. 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.

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PARP1-IN-55

PARP1-IN-55 Chemical Structure

CAS No. : 3109617-69-5

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PARP1-IN-55 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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[1].

IC50 & Target[1]

PARP1

0.019 μM (IC50)

In Vitro

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.

PARP1-IN-55 Related Antibodies

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Induced a significant concentration-dependent increase in the number of nuclear γH2AX fluorescence foci, indicating accumulation of DNA double-strand breaks.

Cell Invasion Assay[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h, 48 h
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.

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h, 48 h
Result: Inhibits the migration of MCF-7 cells in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: MCF-7, L-02 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 14 days
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.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, L-02 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Disrupts the cell membrane integrity of MCF-7 cells, inducing extensive cell death; no effect on the viability of L-02 cells.

Apoptosis Analysis[1]

Cell Line: MCF-7, L-02 cells
Concentration: 3 μM, 5 μM, 10 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Dose-dependently decreased nuclear PARP1 expression and increased γH2AX expression.
Significantly downregulated COL1 expression at 10 μM.
Molecular Weight

429.55

Formula

C25H35NO5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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PARP1-IN-55 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:

PARP1-IN-553109617-69-5PARPDNA/RNA SynthesisReactive Oxygen Species (ROS)Apoptosispoly ADP ribose polymerase PARP1 inhibitorapoptosiselevate ROSdecrease mitochondrial membrane potentialinhibit migration and invasioninhibit colony formationsuppress DNA damage repairbreast cancerMCF-7 cellsAGS cellsSW620 cellsSU-DHL-10 cellsL-02 cellsInhibitorinhibitorinhibit

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