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VU0359595
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VU0359595图片
CAS NO:1246303-14-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
VU0359595 (CID-53361951; ML-270) 是一种有效的选择性药理磷脂酶 D1 (PLD1) 抑制剂,IC50 为 3.7 nM。
Cas No.1246303-14-9
别名CID-53361951,ML-270
化学名(1R,2R)-N-[(1S)-2-[4-(5-bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-2-phenyl-cyclopropanecarboxamide
Canonical SMILESC[C@H](NC([C@@H]1C[C@H]1C2=CC=CC=C2)=O)CN3CCC(N4C(NC5=C4C=CC(Br)=C5)=O)CC3
分子式C25H29BrN4O2
分子量497.4
溶解度≤5mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.