PI3K-IN-41 (compound 2) is a photocaged compound, as well as a photocaged PI3K inhibitor ( IC 50 =18.92 nM) with anticancer properties. PI3K-IN-41 has potential to be used in precisely controlled cancer therapeutics. PI3K-IN-41 exhibits potent PI3K ihibition upon UV light irradiation, and enhances antitumor effect.