VU0359595
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 497.4 |
Cas No. | 1246303-14-9 |
Formula | C25H29BrN4O2 |
Synonyms | CID-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 |
SDF | Download SDF |
Canonical SMILES | C[C@H](NC([C@@H]1C[C@H]1C2=CC=CC=C2)=O)CN3CCC(N4C(NC5=C4C=CC(Br)=C5)=O)CC3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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