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

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 DNA gyrase

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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].
Cellular Effect
Cell Line Type Value Description References
A549 IC50
9.48 μM
Compound: B6
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38554475]
HGC-27 IC50
2.49 μM
Compound: B6
Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38554475]
HeLa IC50
7.21 μM
Compound: B6
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38554475]
HepG2 IC50
3.8 μM
Compound: B6
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38554475]
L02 IC50
> 64 μM
Compound: B6
Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38554475]
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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