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    PARP-IN-1 (3-aminobenzamide; 3-ABA; 3-AB)
    PARP-IN-1 (3-aminobenzamide; 3-ABA; 3-AB)

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    InvivoChem Cat #: V0306
    CAS #: 3544-24-9Purity ≥98%

    Description: PARP-IN-1 (3-Aminobenzamide; 3-ABA; 3-AB) is a novel and potent inhibitor of PARP [ Poly(ADP-ribose)polymerase] with potential anticancer activity. It inhibits PARP with IC50 of<50 nM in CHO cells. It shows potent antiproliferative activity against various cancer cells and high in vivo antitumor efficacy as well. In rodent and human fibroblast cell lines, INO-1001 significantly inhibited PARP activity. Treatment of 10 μM INO-1001 and a single dose of radiation caused significant radiosensitization of the three cells lines. While apoptosis was not increased, suggesting that INO-1001 increased radiation-induced cell killing through interfering with DNA repair mechanisms, increasing necrotic cell death .

    References: Cancer Lett. 2004 Mar 18;205(2):155-60; J Neurotrauma. 2007 Aug;24(8):1399-405. 

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    Molecular Weight (MW)136.15
    FormulaC₇H₈N₂O
    CAS No.3544-24-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: N/A
    H2O:  ≥ 11.11 mg/mL
    Ethanol: N/A
    Synonyms3-Aminobenzamide; PARP-IN-1; 3-ABA; 3-AB


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    In Vitro

    In vitro activity: 3-Aminobenzamide (>1 μM) causes more than 95% inhibition of PARP activity without significant cellular toxicity. INO-1001 significantly sensitizes CHO cells by blocking most of the DNA repair occurring between radiation fractions. 3-Aminobenzamide significantly improves endothelial function by enhancing the acetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400 μM H2O2


    Kinase Assay: PARP activity is measured with a PARP Activity Assay Kit. This method measures relative PARP activity by determining the level of incorporation of 3H-NAD into trichloroacetic acid (TCA) precipitable material in the presence of sheared genomic DNA, which activates PARP. The reaction mixture is added directly to washed cultures in 12-well culture plates and the reaction is allowed to proceed for 60 minutes at 37°C before the cells are removed mechanically, transferred to a microcentrifuge tube, and precipitated with ice-cold 5% TCA.


    Cell Assay: 3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.

    In VivoIn a db/db (Leprdb/db) mouse model, 3-Aminobenzamide ameliorates diabetes-induced albumin excretion and mesangial expansion, and also decreases diabetes-induced podocyte depletion[3]. 3-Aminobenzamide (1.6 mg/kg via intracerebral injection) prevents NAD+ depletion and improves water maze performance after controlled cortical impact (CCI) in mice
    Animal modelMice
    Formulation & Dosage1.6 mg/kg via intracerebral injection
    References

    [1]. Brock WA, et al. Radiosensitization of human and rodent cell lines by INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase. Cancer Lett. 2004 Mar 18;205(2):155-60.

    [2]. Radovits T, et al. Poly(ADP-ribose) polymerase inhibition improves endothelial dysfunction induced by reactive oxidant hydrogen peroxide in vitro. Eur J Pharmacol. 2007 Jun 14;564(1-3):158-66.

    [3]. Szabo C, et al. Poly(ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice. Diabetes. 2006 Nov;55(11):3004-12.

    [4]. Clark RS, et al. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improves water maze performance after traumatic brain injury in mice. J Neurotrauma. 2007 Aug;24(8):1399-405.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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