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.
- CAS No.: 2255341-36-5
- Formula: C22H26Br2N6O4S2
- Molecular Weight:662.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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PARP-1 64.98 nM (IC50) |
Cdk1/cyclin B |
Bcl-2 |
Bax |
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.
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Cell Line:HCC-1937, Capan-1, MCF-7, PANC-1, A549, H460, CaCo-2, HL-7702
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Concentration:20 μM
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Incubation Time:48 h
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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.
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Cell Line:HCC-1937 cells
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Concentration:1, 5 and 10 μM
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Incubation Time:0.5, 4 and 48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice with HCC-1937 xenograft (female, 5-6 weeks, 18-22 g )[1]
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Dosage:25 mg/kg, 50 mg/kg
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Administration:Orally administration
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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.
Chemical Information
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CAS No. 2255341-36-5
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Molecular Weight 662.42
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Formula C22H26Br2N6O4S2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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