4-amino-1,8-Naphthalimide

A PARP inhibitor

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10mg

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440.00

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50mg

￥2475.00

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￥4362.00

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货号: ajci7764
CAS: 1742-95-6
别名: 4-氨基-1,8-萘二胺,4-Aminonaphthalimide,4-ANI
分子式: C12H8N2O2
分子量: 212.2
纯度: >98%
溶解度: ≤1mg/ml in DMSO;0.3mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

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].

参考文献:
[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.