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VU0359595

Catalog No.
C3919
PLD1 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$106.00
Ship with 5-10 days
10mg
$191.00
Ship with 5-10 days
25mg
$430.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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].

References:
[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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt497.4
Cas No.1246303-14-9
FormulaC25H29BrN4O2
SynonymsCID-53361951,ML-270
Solubility≤5mg/ml in DMSO
Chemical Name(1R,2R)-N-[(1S)-2-[4-(5-bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-2-phenyl-cyclopropanecarboxamide
SDFDownload SDF
Canonical SMILESC[[email protected]](NC([[email protected]@H]1C[[email protected]]1C2=CC=CC=C2)=O)CN3CCC(N4C(NC5=C4C=CC(Br)=C5)=O)CC3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

VU0359595