NU1025

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Technical Data

Molecular Weight 176.17 Storage powder
Formula

C9H8N2O2

in solvent
CAS No. 90417-38-2 Synonyms NSC 696807
Solubility (25°C) * In vitro DMSO 35 mg/mL (198.67 mM)
Ethanol 6 mg/mL warmed (34.05 mM)
Water Insoluble
In vivo 40% PEG 400+saline 18mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 8-hydroxy-2-methylquinazolin-4(3H)-one

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]
Features  

Protocol (Only for 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 Assay: [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 Study: [3]

Animal Models Male Sprague Dawley rats
Formulation 40% PEG 400 in saline
Dosages 3 mg/kg
Administration i.p.
 

References

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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