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VU0359595 is a potent and selective inhibitor of PLD1.

Phospholipase D (PLD) isozymes mediate phospholipid hydrolysis and transphosphatidylation. Until now, two mammalian isoforms of PLD, PLD1, and PLD2, have been identified. It has been identified that PLD has been implicated in a human cancer cell progression, actin cytoskeleton reorganization and cell motility [1].

In vitro: VU0359595 was an inhibitor of PLD1 with an IC50 of 3.7 nM. VU0359595 showed >1,700-fold selectivity over PLD2. The IC50 of was VU0359595 against PLD2 was 6.4 μM [1]. Preliminary evidence has demonstrated that VU0359595 showed no interaction with the catalytic site of PLD, but may bind and inhibit PLD through an allosteric site [1]. At 500 nM, VU0359595 significantly reduced the PLD activity in astroglial cultures from wild-type mice by 58% [2]. In cells stimulated by 1% FCS, VU0359595 decreased cell proliferation in wild-type and PLD2-deficient cells at a concentration of 500 nM [2]. VU0359595 (500 nM) significantly reduced cell growth in cells stimulated by either mitogen [2].

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