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Development of a Selective, Allosteric PLD2 Inhibitor

Development of a Selective, Allosteric PLD2 Inhibitor

Sarah A. Scott, Matthew C. O'Reilly, J. Scott Daniels, Ryan Morrison, Roger Ptak, Eric S. Dawson, Nichole Tower, Julie L. Engers, Darren W. Engers, Thomas Oguin, Paul Thomas, Lucille White, H. Alex Brown, etc.

PMID: 23762931

Abstract:

A diversity-oriented synthesis approach of the neuroleptic drug halopemide, reported to be a phospholipase D2 (PLD2) inhibitor (but later shown to be a dual PLD1/2 inhibitor) afforded ML298 (CID 53393915), a potent, >53-fold PLD2 selective allosteric inhibitor (cellular PLD1, IC50 >20,000 nM, cellular PLD2, IC50 = 355 nM). ML298 displays no inhibition of PLD1, and therefore is an improvement over our first generation PLD2 selective inhibitor, VU0364739 (cellular PLD1, IC50 = 1,500 nM, cellular PLD2, IC50 = 20 nM), as at standard in vitro doses, and in vivo exposure levels, both PLD1 and PLD2 are inhibited. ML298 possesses favorable physiochemical and dystrophia myotonica protein kinase (DMPK) properties, making it a useful tool to probe selective PLD2 function in vitro and in vivo. Data here shows therapeutic relevance in virology and oncology.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1426916020	ML298		1426916-02-0	Price

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