857371P
Avanti
VU0359595
(1R,2R)-N-([S]-1-{4-[5-bromo-2-oxo-2,3-dihydro-1H-benzo(d)imidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxamide, powder
Synonym(s):
EVJ; VU0359595
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About This Item
Empirical Formula (Hill Notation):
C25H29BrN4O2
CAS Number:
Molecular Weight:
497.43
UNSPSC Code:
12352211
NACRES:
NA.25
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Assay
>99% (TLC)
form
powder
packaging
pkg of 1 × 1 mg (857371P-1mg)
manufacturer/tradename
Avanti Research™ - A Croda Brand 857371P
lipid type
bioactive lipids
shipped in
dry ice
storage temp.
−20°C
General description
VU0359595 has been shown to selectively inhibit the PLD1 isoform at nM levels (see data below). **Images added as .gif in folder
Application
VU0359595 has been used as PLD2 (phospholipase D2) inhibitor to quantitatively address functional and molecular aspects of the involvement of PLD-derived phosphatidic acid (PA) in regulated exocytosis and as PLD1 inhibitor to treat the knockout mice to study its effects on them.
Biochem/physiol Actions
VU0359595 helps to block phospholipase D (PLD) which in turn reduces deoxyribonucleoside triphosphate (dNTP) biosynthesis in glioma models.
Packaging
5 mL Amber Glass Screw Cap Vial (857371P-1mg)
Legal Information
Avanti Research is a trademark of Avanti Polar Lipids, LLC
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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The role of phospholipase D in regulated exocytosis
Rogasevskaia TP and Coorssen JR
The Journal of biological chemistry, 290(48), 28683-28696 (2015)
Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas
Mathews TP, et al.
ACS Chemical Biology, 10(5), 1258-1268 (2015)
Binding of PLD2-generated phosphatidic acid to KIF5B promotes MT1-MMP surface trafficking and lung metastasis of mouse breast cancer cells
Wang Z, et al.
Developmental Cell, 43(2), 186-197 (2017)
Jana A Lewis et al.
Bioorganic & medicinal chemistry letters, 19(7), 1916-1920 (2009-03-10)
This Letter describes the synthesis and structure-activity-relationships (SAR) of isoform-selective PLD inhibitors. By virtue of the installation of alternative halogenated piperidinyl benzimidazolone privileged structures, in combination with a key (S)-methyl group, novel PLD inhibitors with low nM potency and unprecedented
Xianping Li et al.
Infection and immunity, 80(1), 429-440 (2011-11-16)
Aspergillus fumigatus is the most prevalent airborne fungal pathogen that induces serious infections in immunocompromised patients. Phospholipases are key enzymes in pathogenic fungi that cleave host phospholipids, resulting in membrane destabilization and host cell penetration. However, knowledge of the impact
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