|4-amino-1,8-Naphthalimide PARP inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||1742-95-6||SDF||Download SDF|
|Solubility||≤1mg/ml in DMSO;0.3mg/ml in dimethyl formamide||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
4-amino-1,8-Naphthalimide is a novel inhibitor of PARP with IC50 value of 180 nM .
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 .
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 .
. 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.
. 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.
. 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.
. 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.