NU1025

Catalog No.S7730 Synonyms: NSC 696807

NU1025 Chemical Structure

Molecular Weight(MW): 176.17

NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

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Biological Activity

Description NU1025 is a potent PARP inhibitor with IC50 of 400 nM.
Targets
PARP [1]
400 nM
In vitro

NU1025 (0.2 mM) treatment attenuates H2O2 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]

Protocol

Kinase Assay:[4]
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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.
Cell Research:[3]
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  • Cell lines: D54 and U251 cells
  • Concentrations: 160 μM
  • Incubation Time: 5 days
  • Method: 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)
Animal Research:[3]
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  • Animal Models: Male Sprague Dawley rats
  • Formulation: 40% PEG 400 in saline
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (198.67 mM)
Ethanol 6 mg/mL warmed (34.05 mM)
Water Insoluble
In vivo Add solvents individually and in order:
40% PEG 400+saline
18mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 176.17
Formula

C9H8N2O2

CAS No. 90417-38-2
Storage powder
Synonyms NSC 696807

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID