Reversible and selective inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50
values are 0.28 and 5.3 μ
M respectively). Displays little affinity for other commonly studied kinases including PI 3-K, ATM and ATR (IC50
values are all > 100 μ
M). Induces apoptosis in vitro
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Selective benzopyranone and pyrimido[2,1-α]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies and radiosensitization of a human tumor cell line in vitro.
Griffen et al.
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)oyrimido[2,1-α]isoquinolin-4-one.
Ballo et al.