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药物的细胞毒性，并具有抗癌和神经保护的作用。
| 生物活性 | NU1025 is a potentPARPinhibitor with anIC50of 400 nM and aKiof 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] |
体外研究
(In Vitro) | NU1025 (0.2 mM) pretreatment restores cell viability to approximately 73% and 82% in H2O2and 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 H2O2and SIN-1 injured cells. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(709.54 mM;Need ultrasonic) 配制储备液 | 1 mM | 5.6763 mL | 28.3817 mL | 56.7634 mL | | 5 mM | 1.1353 mL | 5.6763 mL | 11.3527 mL | | 10 mM | 0.5676 mL | 2.8382 mL | 5.6763 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (11.81 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (11.81 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (11.81 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (11.81 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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