4-amino-1,8-Naphthalimide

4-amino-1,8-Naphthalimide

Catalog Number:
L002372994APE
Mfr. No.:
APE-C4310
Price:
$405
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      • Overview
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          Background

          4-amino-1,8-Naphthalimide is a novel inhibitor of PARP with IC50 value of 180 nM [1][3].
          The poly(ADP-ribose) polymerases (PARPs) is a nuclear enzyme that catalyzes a transfer of the ADP-ribose moiety of NAD+ to acceptor protein with a concomitant release of nicotinamide. PARPs play important roles in DNA repair, cell differentiation, control of cell cycle, transformation, transcription, and alteration of chromatin architecture [2][3][4].
          4-amino-1,8-Naphthalimide (4-ANI) is a novel PARP inhibitor and a radiation sensitizer. In exponentially growing hamster lung fibroblasts (V79), rat prostate carcinoma (R3327-AT1) and human prostate carcinoma (DU145) cells, 4-ANI significantly potentiated the cytotoxicity of gamma-irradiation in a dose dependent way and is not cytotoxic in the absence of radiation. 4-ANI was used to study the role of PARP activity in a variety of cell systems [1][3].

          [1]. Schlicker A, Peschke P, Bürkle A, et al. 4-Amino-1,8-naphthalimide: a novel inhibitor of poly(ADP-ribose) polymerase and radiation sensitizer. Int J Radiat Biol. 1999 Jan;75(1):91-100.
          [2]. Davar D1, Beumer JH, Hamieh L, et al. Role of PARP inhibitors in cancer biology and therapy. Curr Med Chem. 2012;19(23):3907-21.
          [3]. Banasik M, Komura H, Shimoyama M,et al. Specific inhibitors of poly(ADP-ribose) synthetase and mono(ADP-ribosyl)transferase. J Biol Chem. 1992 Jan 25;267(3):1569-75.
          [4]. Issaeva N, Thomas HD, Djureinovic T, et al. 6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 2010 Aug 1;70(15):6268-76.

      • Properties
        • Alternative Name
          4-Aminonaphthalimide,4-ANI; 6-amino-1H-benz[de]isoquinoline-1,3(2H)-dione
          CAS Number
          1742-95-6
          Molecular Formula
          C12H8N2O2
          Molecular Weight
          212.2
          Appearance
          A crystalline solid
          Purity
          Purity ≥ 95.00%
          Solubility
          ≤1mg/ml in DMSO;0.3mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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