For research purposes only

Cat. No BA142114783

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Description of biological activity

NU7163 (IC50 = 0.19 μM) is selective ATP-competitive DNA-PK inhibitior, with a Ki value of 24 nM. It exhibits selectivity for DNA-PK compared with the related enzymes ATM, ATR, mTOR, and PI3Ks. NU7163 sensitized the HeLa human tumor cell line to the cytotoxic effects of ionizing radiation in vitro, a dose modification factor of 2.3 at 10% survival being observed with an inhibitor concentration of 5 μM [2]
IC50: 0.19μM (DNA-PK), 2.4 μM (PI3Kα) [1]
Target: DNA-dependent protein kinase (DNA-PK), Phosphatidylinositol 3-Kinase α (PI3Kα)

Biological target category

Phosphatidylinositol 3-kinase-related kinases (PIKKs), Phosphoinositide 3-kinases PI3K(s)

TECHNICAL INFORMATION

2-(4-methylmorpholin-4-yl)benzo[h]chromen-4-one Phosphatidylinositol 3-Kinase α (PI3Kα) inhibitor.

IUPAC Name: 2-(4-methylmorpholin-4-yl)benzo[h]chromen-4-one

Chemical Formula: C18H17NO3

CAS Number: 503468-03-9

Molecular Weight: 295.340

Purity: > 97% chemical purity (LCMS)

Solubility: 5mM in DMSO

1H-NMR spectrum (click to enlarge)

REFERENCES

[1] RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK. INHIBITORS OF MTOR AND METHODS OF TREATMENT USING SAME. WO2008/148074 A2, 2008

[2] Griffin RJ, et al. Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. J Med Chem. 2005 Jan 27;48(2):569-85.

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