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%.

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

TOPOI/PARP-1-IN-1 Chemical Structure

TOPOI/PARP-1-IN-1 Chemical Structure

CAS No. : 2948352-16-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

TOPOI/PARP-1-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

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

View All Topoisomerase Isoform Specific Products:

View All Isoforms
Topoisomerase Topo I Topo II

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

TOPOI/PARP-1-IN-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TOPOI/PARP-1-IN-1
Cat. No.:
HY-158138
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.