NU1025 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。
产品描述
NU1025 is a potent PARP inhibitor with IC50 of 400 nM.
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
Treatment with NU1025 (1 and 3 mg/kg) reduces the infarction to 25% and 45% versus vehicle treated rats, respectively. NU1025 (1 and 3 mg/kg) treatment significantly reduces edema volume. NU1025 also produces significant improvement in neurological deficits.[2]
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.
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)
Cas No.
90417-38-2
分子式
C9H8N2O2
分子量
176.175
别名
NSC 696807
储存和溶解度
DMSO:17.6 mg/mL (100 mM)
1eq. NaOH:17.6 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
