NU 7026

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Cat.No. 2828 - NU 7026 | C17H15NO3 | CAS No. 154447-35-5
Description: Selective DNA-PK inhibitor
Chemical Name: 2-(4-Morpholinyl)-4H-naphthol[1,2-b]pyran-4-one
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Literature

Biological Activity

ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK). Displays selectivity over other PIKK family enzymes (IC50 values are 0.23, 13.0, > 100 and > 100 μM for DNA-PK, PI3K, ATM and ATR respectively). Radiosensitizes both proliferating and quiescent mouse embryonic fibroblast cells to IR and inhibits DSB repair.

Technical Data

M. Wt 281.31
Formula C17H15NO3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 154447-35-5
PubChem ID 9860529
InChI Key KKTZALUTXUZPSN-UHFFFAOYSA-N
Smiles O=C2C1=CC=C3C(C=CC=C3)=C1OC(N4CCOCC4)=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.81 10

Preparing Stock Solutions

The following data is based on the product molecular weight 281.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.55 mL 17.77 mL 35.55 mL
5 mM 0.71 mL 3.55 mL 7.11 mL
10 mM 0.36 mL 1.78 mL 3.55 mL
50 mM 0.07 mL 0.36 mL 0.71 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Veuger et al (2003) Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-I. Cancer Res. 63 6008 PMID: 14522929

Amrein et al (2007) Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. J.Pharmacol.Exp.Ther. 321 848 PMID: 17351105

Hollick et al (2003) 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase (DNA-PK). Bioorg.Med.Chem.Letts. 13 3083 PMID:


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View all DNA-Dependent Protein Kinase Inhibitors

Keywords: Selective DNA-dependent protein kinases inhibitors inhibits DNA-PK NU7026 DNA-dependent Protein Kinase

6 Citations for NU 7026

Citations are publications that use Tocris products. Selected citations for NU 7026 include:

You et al (2015) Nanoparticulate carbon black in cigarette smoke induces DNA cleavage and Th17-mediated emphysema. Elife 4 PMID: 26437452

Dolman et al (2015) DNA-Dependent Protein Kinase As Molecular Target for Radiosensitization of Neuroblastoma Cells. PLoS One 10 e0145744 PMID: 26716839

Nakahara et al (2015) Activation of NF-κB by human papillomavirus 16 E1 limits E1-dependent viral replication through degradation of E1. Chembiochem 89 5040 PMID: 25717108

Fard et al (2013) The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway. Cell Cycle 13 408 PMID: 24247150

Tang et al (2012) Detection of early Abl kinase activation after ionizing radiation by using a peptide biosensor. J Neurosci 13 665 PMID: 22334513

Bohgaki et al (2011) Genomic instability, defective spermatogenesis, immunodeficiency, and cancer in a mouse model of the RIDDLE syndrome. PLoS Genet 7 e1001381 PMID: 21552324


Do you know of a great paper that uses NU 7026 from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for NU 7026

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