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CAS No. : 90417-38-2
MCE 国际站:NU1025
产品活性:NU1025 是一种有效的 PARP 抑制剂,IC50 为 400 nM,Ki 为 48 nM。NU1025 可增强电离辐射和抗癌活性分子的细胞毒性,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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