1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. PARP DNA/RNA Synthesis Apoptosis CDK Bcl-2 Family
  3. PARP1-IN-50

PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer.

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

PARP1-IN-50

PARP1-IN-50 Chemical Structure

CAS No. : 2255341-36-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer[1].

IC50 & Target[1]

PARP-1

64.98 nM (IC50)

Cdk1/cyclin B

 

Bcl-2

 

Bax

 

In Vitro

PARP1-IN-50 (Compound 13) demonstrates significant antiproliferative activity in HCC-1937, Capan-1, MCF-7 and PANC-1 cells with an IC50 of 0.88, 0.56, 4.49 and 1.53 μM[1].
PARP1-IN-50 (1-10 μM, 48 h) induces G2/M arrest and inhibits the expression levels of CDK1 and cyclin B in HCC-1937 cells[1].
PARP1-IN-50 (1-10 μM, 4 h) inhibits H2O2-induced PAR formation in HCC-1937 cells[1].
PARP1-IN-50 (1-10 μM, 30 mins) increases PARP-1-DNA trapping and induces DNA double strand breaks in HCC-1937 cells[1].
PARP1-IN-50 (1-10 μM, 48 h) induces apoptosis in HCC-1937 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: HCC-1937, Capan-1, MCF-7, PANC-1, A549, H460, CaCo-2, HL-7702
Concentration: 20 μM
Incubation Time: 48 h
Result: Showed an inhibition rate of 100% in SK-OV-3 cells, 84.36% in PANC-1, 44.68% in H460 cells, 75.89 % in HL-7702 cells and 68.33% in MCF-7 cells.

Western Blot Analysis[1]

Cell Line: HCC-1937 cells
Concentration: 1, 5 and 10 μM
Incubation Time: 0.5, 4 and 48 h
Result: Inhibited PAR levels and increased the PARP-1-DNA trapping levles.
Increased γ-H2AX protein levels.
Reduced CDK1 and cyclin B levles.
Upregulated the expression of Bax and downregulated the expression of Bcl-2.
In Vivo

PARP1-IN-50 (Compound 13) (25-50 mg/kg, p.o., daily for 21 days) significantly inhibits HCC-1937 xenograft tumor growth with a favorable safety profile in BALB/c nude mice[1].

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

Animal Model: BALB/c nude mice with HCC-1937 xenograft (female, 5-6 weeks, 18-22 g )[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Orally administration
Result: Showed growth inhibition rates of 53.5% and 71.4% at 25 mg/kg and 50 mg/kg.
Reduced tumor weight and volume.
Had no significant changes in body weight and no significant organ toxicity.
Reduced Ki67 expression and increased γ-H2AX expression.
Molecular Weight

662.42

Formula

C22H26Br2N6O4S2

CAS No.
SMILES

NC(N/N=C/C1=CC(Br)=C(OCCCCOC2=C(C=C(C=C2Br)/C=N/NC(N)=S)OC)C(OC)=C1)=S

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.
  • 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PARP1-IN-50
Cat. No.:
HY-179614
Quantity:
MCE Japan Authorized Agent: