| Name | NU1025 |
| Description | NU1025 (NSC-696807) is a potent PARP inhibitor with IC50 of 400 nM. |
| Cell Research | 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) |
| Kinase Assay | 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. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 40 mg/mL (227.05 mM), Sonication is recommended.
1eq. NaOH : 17.6 mg/mL (100 mM)
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| Keywords | repair | anti-cancer | NU1025 | cytotoxicity | PARP | inhibit | NU 1025 | DNA | NSC-696807 | NU-1025 | Inhibitor | PAR | Neuroprotective | NSC696807 | NAD | poly ADP ribose polymerase |
| Inhibitors Related | 4'-Methoxychalcone | Niraparib tosylate monohyrate | VPC-70063 | 3-Aminobenzamide | XAV-939 | Niraparib | 3-Methoxybenzamide | Talazoparib | Olaparib | Benzamide | Picolinamide | OUL35 |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Neuroprotective Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Active Compound Library |
United States
