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-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.

For research use only. We do not sell to patients.

PARP1-IN-49

PARP1-IN-49 Chemical Structure

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PARP1-IN-49 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-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[1].

IC50 & Target[1]

PARP1

23.56 nM (IC50)

PARP1

17.78 nM (Kd)

PARP2

285.39 nM (IC50)

In Vitro

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.

PARP1-IN-49 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: Inhibited cell proliferation and migration in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
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.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: Induced DNA damage and the accumulation of double-strand breaks, as indicated by increased γH2AX and comet tail length.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
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%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: The proportion of cells undergoing early and late apoptosis increased from 0.49% to 53.8%. 
Parmacokinetics
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
In Vivo

PARP1-IN-49 (compound 9a) (20, 40 mg/kg; Intraperitoneal; 22 days) significantly inhibits tumor growth in MDA-MB-231 cells subcutaneously inoculated into BALB/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 20 mg/kg, 40 mg/kg
Administration: Intraperitoneal; 22 days
Result: Tumor growth was significantly inhibited.
Molecular Weight

286.26

Formula

C15H11FN2O3
SMILES

O=C(NC)C1=CC(C2=CC=C(OC(N3)=O)C3=C2)=CC(F)=C1
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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PARP1-IN-49 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-49PARPDNA/RNA SynthesisReactive Oxygen Species (ROS)Apoptosispoly ADP ribose polymerase PARP1Inhibitorinhibitorinhibit

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