Product Introduction
Bioactivity


英文名: NU1025

描述: NU1025 (NSC-696807) 是一种PARP 的有效抑制剂，IC50为 400 nM，Ki 为 48 nM。它可增强电离辐射和抗癌药物的细胞毒性，有抗癌和神经保护的作用。

细胞实验: Cells are seeded in 96-well plates at a density of 2,500 cells/well and treated with the indicated doses of NU1025. Adherent cells are irradiated in medium with 250 kVp X-rays (dose rate 0.5 Gy/min). Untreated cells are used as a control. Following an up to 5 day incubation, cell proliferation is assessed by MTT assay.(Only for Reference)

激酶实验: PARP activation assay: Cells are suspended in hypotonic buffer (9 mM HEPES, pH 7.8, 4.5% (v/v) dextran, 4.5 mM MgCl2 and 5 mM DTT) at 1.5 × 107/mL on ice for 30 min, then 9 vol of isotonic buffer (40 mM HEPES, pH 7.8, 130 mM KCl, 4% (v/v) dextran, 2 mM EGTA, 2.3 mM MgCl2, 225 mM sucrose and 2.5 mM DTT) is added. The reaction is started by adding 300 μL cells to 100 μL 300 μM NAD+ containing [32P]-NAD+, and terminated by the addition of 2 mL ice-cold 10% (w/v) TCA +10% (w/v) sodium pyrophosphate. After 30 min on ice the precipitated 32P-labelled ADP-ribose polymers are filtered, washed five times with 1% (v/v) TCA, 1% (v/v) sodium pyrophosphate, dried and counted.

体外活性: NU1025 (0.2 mM) treatment attenuates Water2 induced cytotoxicity. NU1025 per se does not have any effect on cell viability. NU1025 pretreatment significantly increases cell viability (82.59 4.67%) in SIN-1 (0.8 mM) exposed cells.[2] NU1025 has no detectable effect on the proliferation of D54 and U251 cells. Treatment with NU1025 markedly inhibits the enhanced activation of PARP-1 induced by TPT and RT treatment.[3] No DNA strand breakage is detected following exposure to 200 μM NU1025 alone.[4]

体内活性: 使用NU1025（1和3 mg/kg）处理，与对照组大鼠相比，可将梗塞面积减少至25%和45%。NU1025（1和3 mg/kg）治疗显著减少了水肿体积。此外，NU1025还显著改善了神经功能缺损。[2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 17.6 mg/mL (100 mM)
1eq. NaOH : 17.6 mg/mL (100 mM)


关键字: repair | anti-cancer | NU1025 | cytotoxicity | PARP | inhibit | NU 1025 | DNA | NSC-696807 | NU-1025 | Inhibitor | PAR | Neuroprotective | NSC696807 | NAD | poly ADP ribose polymerase

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相关库: Anti-Aging Compound Library | Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | NO PAINS Compound Library