NU1025

NU1025 is a potent PARP inhibitor with an IC₅₀ of 400 nM and a K_i of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity^[1][2][3]. IC50 & Target: IC50: 400 nM (PARP)^[2]
Ki: 48 nM (PARP)^[3] 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]. 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].