NU1025

Catalog No.S7730 Synonyms: NSC 696807

For research use only.

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

NU1025 Chemical Structure

CAS No. 90417-38-2

Selleck's NU1025 has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description NU1025 (NSC 696807) 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 (from reference)

Kinase Assay:[4]
  • 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]
  • 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.
Animal Research:[3]
  • Animal Models: Male Sprague Dawley rats
  • Dosages: 3 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 35 mg/mL
(198.67 mM)
Water Insoluble
Ethanol '6 mg/mL warmed

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
40% PEG 400+saline
For best results, use promptly after mixing.

18mg/mL

Chemical Information

Molecular Weight 176.17
Formula

C9H8N2O2

CAS No. 90417-38-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC2=C(C=CC=C2O)C(=O)N1

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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