2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP Topoisomerase Apoptosis
  4. TOPOI/PARP-1-IN-1

TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%.

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TOPOI/PARP-1-IN-1 Chemical Structure

TOPOI/PARP-1-IN-1 Chemical Structure

CAS No. : 2948352-16-5

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TOPOI/PARP-1-IN-1 Related Antibodies

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Topoisomerase Topo I Topo II

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Description

TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%[1].

IC50 & Target

IC50: 0.09 μM (PARP1)[1].
In Vitro

TOPOI/PARP-1-IN-1 (1.25-5 μM; 48 h) inhibits the proliferation and migration of HGC-27 cells in a dose-dependent manner[1].
TOPOI/PARP-1-IN-1 (1.25-5 μM; 24 h) induces apoptosis in a dose-dependent manner in HGC-27 cells[1].
TOPOI/PARP-1-IN-1 induces DNA damage and decreases TOPOI expression in HGC-27 cells[1].
TOPOI/PARP-1-IN-1 exhibits anti-tumor activity, with IC50 values of 7.21 μM, 9.48 μM, 3.80 μM and 2.49 μM against HeLa, A549, HepG-2 and HGC-27 cells, respectively[1].

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

TOPOI/PARP-1-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HGC-27 cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 48 h
Result: Demonstrated dose-dependent inhibitory effect of B6 on the clonogenicity of HGC-27 cells.

Apoptosis Analysis[1]

Cell Line: HGC-27 cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 24 h
Result: Induced 15.5%, 43.1% and 76.0% of cell apoptosis when the concentrations were 1.25, 2.5, and 5 μM respectively.
In Vivo

TOPOI/PARP-1-IN-1 (40 mg/kg; p.o.; once every two days, for a total of 17 days) inhibits HGC-27 tumor growth in xenograft tumor mice model[1].

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

Animal Model: Female BALB/c nude mice (xenograft tumor model of HGC-2 cells)[1].
Dosage: 40 mg/kg
Administration: Oral administration; once every two days, for a total of 17 days
Result: Exhibited tumor growth inhibition rate (TGI) of 75.4% in mice.
Molecular Weight

718.52

Formula

C36H38Br2N4O2
CAS No.
SMILES

O=C(N([C@@]([H])([C@]1(CCCN2CCC3)[H])CCCC4=NC(C=C(C(Br)=C5)Br)=C5N4)C[C@@]3([H])[C@@]12[H])OCC6C7=C(C8=C6C=CC=C8)C=CC=C7
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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TOPOI/PARP-1-IN-1 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:

TOPOI/PARP-1-IN-12948352-16-5PARPTopoisomeraseApoptosispoly ADP ribose polymerase HGC-27cancertumorHeLaA549HepG-2apoptosisTGIInhibitorinhibitorinhibit

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