NU1025

Synonyms: NSC 696807

NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.

NU1025 Chemical Structure

NU1025 Chemical Structure

CAS: 90417-38-2

Selleck's NU1025 has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.29%
99.29

NU1025 Related Products

Signaling Pathway

Choose Selective PARP Inhibitors

Biological Activity

Description NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
Targets
PARP [1]
400 nM
In vitro
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]
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.
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Male Sprague Dawley rats
Dosages 3 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 176.17 Formula

C9H8N2O2

CAS No. 90417-38-2 SDF Download NU1025 SDF
Smiles CC1=NC2=C(C=CC=C2O)C(=O)N1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 35 mg/mL ( (198.67 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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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