NU 7026

• CAT Number: I001949
• CAS Number: 154447-35-5
• Molecular Formula: C17H15NO3
• Molecular Weight: 281.31
• Purity: ≥95%
• Synonyms: 2-morpholin-4-ylbenzo[h]chromen-4-one
• Target: DNA-PK
• Solubility: DMSO: 1 mg/mL, H2O: < 1 mg/mL
• Storage: 2-8°C
• IC50: 0.23 uM [1]
• InChI: InChI=1S/C17H15NO3/c19-15-11-16(18-7-9-20-10-8-18)21-17-13-4-2-1-3-12(13)5-6-14(15)17/h1-6,11H,7-10H2
• InChIKey: KKTZALUTXUZPSN-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=CC(=O)C3=C(O2)C4=CC=CC=C4C=C3

NU7026（Cat No.:I001949）, also known as LY293646 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK). It exhibits an IC50 value of 0.23μM in cell-free assays, displaying 60 times greater selectivity for DNA-PK compared to PI3K. Notably, NU7026 does not inhibit ATM and ATR, two other important kinases involved in DNA damage response pathways. By targeting DNA-PK, NU7026 enhances cell cycle arrest at the G2/M phase and induces apoptosis, making it a valuable tool for studying DNA repair processes and exploring potential therapeutic applications in cancer treatment.

Reference

[1]. Hollick JJ, Golding BT, Hardcastle IR, 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK). Bioorg Med Chem Lett. 2003 Sep 15;13(18):3083-6.
[2]. Amrein L, Loignon M, Goulet AC, 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. 2007 Jun;321(3):848-55.
[3]. Veuger SJ, Curtin NJ, Richardson CJ, Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15.
[4]. Urushihara Y, Kobayashi J, Matsumoto Y, DNA-PK inhibition causes a low level of H2AX phosphorylation and homologous recombination repair in Medaka (Oryzias latipes) cells. Biochem Biophys Res Commun. 2012 Dec 14;429(3-4):131-6.
[5]. Nutley BP, Smith NF, Hayes A, Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026. Br J Cancer. 2005 Oct 31;93(9):1011-8.