2. Academic Validation
  3. Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release

Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release

  • ACS Med Chem Lett. 2023 Jul 24;14(8):1100-1107. doi: 10.1021/acsmedchemlett.3c00240.
Hua Tian 1 2 3,  Shen You 1 3,  Tianning Xiong 1 2 3,  Ming Ji 1 3,  Kehui Zhang 1 2 3,  Lin Jiang 1 2 3,  Tingting Du 1 3,  Ying Li 1 2 3,  Wenqian Liu 1 2 3,  Songwen Lin 1 2 3,  Xiaoguang Chen 1 3,  Heng Xu 1 2 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • 2 Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • 3 Key Laboratory of Small Molecule Immuno-Oncology Drug Discovery, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
PMID: 37583818 DOI: 10.1021/acsmedchemlett.3c00240
Abstract

A novel photocaged PI3K Inhibitor 2 was designed and synthesized by introducing a cascade photocaging group to block its key interaction with the kinase. Upon UV LIGHT irradiation, the photocaged compound released a highly potent PI3K Inhibitor to recover its Anticancer properties and a Fluorescent Dye for real-time reporting of drug release, providing a new approach for studying the PI3K signaling transduction pathway as well as developing precisely controlled Cancer therapeutics.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-155730
    PI3K Inhibitor