Discovery - University of Dundee - Online Publications

Library & Learning Centre

Characterization of TAE684 as a potent LRRK2 kinase inhibitor

Characterization of TAE684 as a potent LRRK2 kinase inhibitor

Research output: Contribution to journalArticle

View graph of relations


  • Jinwei Zhang
  • Xianming Deng
  • Hwan Geun Choi
  • Dario R. Alessi (Lead / Corresponding author)
  • Nathanael S. Gray (Lead / Corresponding author)

Research units


Original languageEnglish
Pages (from-to)1864-1869
Number of pages6
JournalBioorganic & Medicinal Chemistry Letters
Issue number5
Early online date28 Jan 2012
StatePublished - 1 Mar 2012


Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC50 of 7.8 nM against wild-type LRRK2, 6.1 nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 mu M in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10 mg/kg. (c) 2012 Elsevier Ltd. All rights reserved.



Library & Learning Centre

Contact | Accessibility | Policy