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关于此项目
经验公式(希尔记法):
C25H29BrN4O2
化学文摘社编号:
分子量:
497.43
MDL number:
UNSPSC Code:
12352211
NACRES:
NA.25
产品名称
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
InChI key
JSVNNLRZCJAYTQ-ORYQWCPZSA-N
SMILES string
Brc1cc2[nH][c]([n](c2cc1)C3CCN(CC3)C[C@@H](NC(=O)[C@H]4[C@@H](C4)c5ccccc5)C)=O
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
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.
General description
VU0359595 has been shown to selectively inhibit the PLD1 isoform at nM levels (see data below). **Images added as .gif in folder
Packaging
5 mL Amber Glass Screw Cap Vial (857371P-1mg)
Legal Information
Avanti Research is a trademark of Avanti Polar Lipids, LLC
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas
Mathews TP, et al.
ACS Chemical Biology, 10(5), 1258-1268 (2015)
The role of phospholipase D in regulated exocytosis
Rogasevskaia TP and Coorssen JR
The Journal of biological chemistry, 290(48), 28683-28696 (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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