VU0359595

- Overview
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    Background
    
    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].
    
    [1] Lewis J A, Scott S A, Lavieri R, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity[J]. Bioorganic & medicinal chemistry letters, 2009, 19(7): 1916-1920.
    [2] Burkhardt U, Beyer S, Klein J. Role of phospholipases D1 and 2 in astroglial proliferation: effects of specific inhibitors and genetic deletion[J]. European journal of pharmacology, 2015, 761: 398-404.
- Properties
  - Alternative Name
    
    CID-53361951,ML-270; (1R,2R)-N-[(1S)-2-[4-(5-bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-2-phenyl-cyclopropanecarboxamide
    
    CAS Number
    
    1246303-14-9
    
    Molecular Formula
    
    C25H29BrN4O2
    
    Molecular Weight
    
    497.4
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    ≤5mg/ml in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

VU0359595

Background

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