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Cat. No.: HY-158138

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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%.

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

CAS No.: 2948352-16-5
Formula: C₃₆H₃₈Br₂N₄O₂
Molecular Weight:718.52

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

TOPOI/PARP-1-IN-1 Chemical Structure

CAS No.: 2948352-16-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 0.09 μM (PARP1)^[1].

All PARP Isoforms :

All Topoisomerase Isoforms :

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]
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]
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]
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.

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.

Chemical Information

CAS No. 2948352-16-5
Molecular Weight 718.52
Formula C₃₆H₃₈Br₂N₄O₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Qiu G, et al. Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy. Eur J Med Chem. 2024 Mar 27;270:116348. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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TOPOI/PARP-1-IN-1

All PARP Isoforms

All Topoisomerase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

TOPOI/PARP-1-IN-1 Related Classifications

HY-158138 Related Classifications