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NU1025

CAS No. : 90417-38-2

MCE 站：NU1025

产品活性：NU1025 是一种有效的 PARP 抑制剂，IC₅₀ 为 400 nM，K_i 为 48 nM。NU1025 可增强电离辐射和抗癌药物的细胞毒性，并具有抗癌和神经保护的作用。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: NU1025 (0.2 mM) pretreatment restores cell viability to approximately 73% and 82% in H₂O₂ and SIN-1 injured cells, respectively.
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.

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.

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