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4-amino-1,8-Naphthalimide

产品信息
  • 规格:10mg产品价格:420
    规格:50mg产品价格:1900
    规格:100mg产品价格:3360
    规格:250mg产品价格:7360
    Catalog Number GC11761
    Synonyms 4-Aminonaphthalimide,4-ANI
    Molecular Formula C12H8N2O2
    Relative Molecular Mass 212.2
    CAS Registry Number 1742-95-6
    Formulation A solid
    Purity ≥98%
    Storage Store at -20°C
    SMILES NC1=C2C(C3=CC=C2)=C(C=C1)C(NC3=O)=O
    产品描述
    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].References:[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.
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