NU1025

Cas No.:	90417-38-2
Chemical Name:	8-​hydroxy-​2-​methyl-​4(3H)-​quinazolinone
Synonyms:	NU 1025，NU 1025
SMILES:	CC1=NC(=O)C2=C(N1)C(=CC=C2)O
Formula:	C9H8N2O2
M.Wt:	176.2
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].
Target:	IC50: 400 nM (PARP)[2] Ki: 48 nM (PARP)[3]
In Vivo:	NU1025 (1-3 mg/kg; intraperitoneal injection; male Sprague Dawley rats) treatment at 1 and 3 mg/kg reduces total infarct volume to 25% and 45%, respectively, when administered 1 h before reperfusion. NU1025 also produces significant improvement in neurological deficits. Neuroprotection with NU1025 is associated with reduction in PAR accumulation, reversal of brain NAD depletion and reduction in DNA fragmentation[1]. Animal Model: Male Sprague Dawley rats (250-270 g) induced focal cerebral ischemia[1] Dosage: 1 mg/kg, 3 mg/kg Administration: Intraperitoneal injection Result: At 1 and 3 mg/kg, reduced total infarct volume to 25% and 45%, respectively.
In Vitro:	NU1025 (0.2 mM) pretreatment restores cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells, respectively[1]. NU1025 enhances the cytotoxicity of the DNA-methylating agent MTIC, γ-irradiation and bleomycin 3.5-, 1.4- and 2-fold respectively in L1210 cells. The recovery from potentially lethal γ-irradiation damage cytotoxicity in plateau-phase cells is also inhibited by NU 1025. NU1025 causes a marked retardation of DNA repair[2]. Cell Viability Assay[1] Cell Line: PC12 cells Concentration: 0.2 mM Incubation Time: 6.5 hours Result: Restored cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells.
References:	[1]. Kaundal RK, et al. Neuroprotective effects of NU1025, a PARP inhibitor in cerebral ischemia are mediated through reduction in NAD depletion and DNA fragmentation. Life Sci. 2006 Nov 10;79(24):2293-302. [2]. Bowman KJ, et al. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. Br J Cancer. 1998 Nov;78(10):1269-77. [3]. Delaney CA, et al. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Clin Cancer Res. 2000 Jul;6(7):2860-7.