1426916-23-5Relevant articles and documents
Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-triazaspiro[4.5]decane core: Discovery of ML298 and ML299 that decrease invasive migration in U87-MG glioblastoma cells
O'Reilly, Matthew C.,Scott, Sarah A.,Brown, Kyle A.,Oguin, Thomas H.,Thomas, Paul G.,Daniels, J. Scott,Morrison, Ryan,Brown, H. Alex,Lindsley, Craig W.
, p. 2695 - 2699 (2013/05/22)
An iterative parallel synthesis effort identified a PLD2 selective inhibitor, ML298 (PLD1 IC50 > 20 000 nM, PLD2 IC50 = 355 nM) and a dual PLD1/2 inhibitor, ML299 (PLD1 IC50 = 6 nM, PLD2 IC50 = 20 nM). SAR studies revealed that a small structural change (incorporation of a methyl group) increased PLD1 activity within this classically PLD2-preferring core and that the effect was enantiospecific. Both probes decreased invasive migration in U87-MG glioblastoma cells.