VU 0155069Potent and selective PLD1 inhibitor CAS# 1130067-06-9 |
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| Cas No. | 1130067-06-9 | SDF | Download SDF |
| PubChem ID | 56972237 | Appearance | Powder |
| Formula | C26H28Cl2N4O2 | M.Wt | 499.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 50 mM in ethanol | ||
| Chemical Name | N-[(2S)-1-[4-(5-chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]propan-2-yl]naphthalene-2-carboxamide;hydrochloride | ||
| SMILES | CC(CN1CCC(CC1)N2C3=C(C=C(C=C3)Cl)NC2=O)NC(=O)C4=CC5=CC=CC=C5C=C4.Cl | ||
| Standard InChIKey | RQULTQQAHGYYDG-LMOVPXPDSA-N | ||
| Standard InChI | InChI=1S/C26H27ClN4O2.ClH/c1-17(28-25(32)20-7-6-18-4-2-3-5-19(18)14-20)16-30-12-10-22(11-13-30)31-24-9-8-21(27)15-23(24)29-26(31)33;/h2-9,14-15,17,22H,10-13,16H2,1H3,(H,28,32)(H,29,33);1H/t17-;/m0./s1 | ||
| General tips | For 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective phospholipase D1 (PLD1) inhibitor (IC50 values are 46 and 933 nM for PLD1 and PLD2 respectively). Inhibits migration of human and mouse breast cancer cell lines in transwell assays. |
VU 0155069 Dilution Calculator
VU 0155069 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0023 mL | 10.0114 mL | 20.0228 mL | 40.0457 mL | 50.0571 mL |
| 5 mM | 0.4005 mL | 2.0023 mL | 4.0046 mL | 8.0091 mL | 10.0114 mL |
| 10 mM | 0.2002 mL | 1.0011 mL | 2.0023 mL | 4.0046 mL | 5.0057 mL |
| 50 mM | 0.04 mL | 0.2002 mL | 0.4005 mL | 0.8009 mL | 1.0011 mL |
| 100 mM | 0.02 mL | 0.1001 mL | 0.2002 mL | 0.4005 mL | 0.5006 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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[Lessons learned from the evacuation of the VU University Medical Centre after flooding].[Pubmed:28224872]
Ned Tijdschr Geneeskd. 2017;161:D861.
On 8 September 2015, flooding of the lower floors of the VU University Medical Center in Amsterdam caused serious damage to many vital technical services, such as water and power supplies. The decision was made to completely evacuate the university hospital. This paper describes the chronology and events of that day and shares a number of important lessons that were learned, in order to help readers to optimise crisis organisation in their own institutions. A serious situation or disaster can never be standardised in protocols or manuals; flexibility, improvisation and confidence in one another's expertise and commitment are therefore essential.
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.[Pubmed:19268584]
Bioorg Med Chem Lett. 2009 Apr 1;19(7):1916-20.
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 levels of PLD1 isoform selectivity (approximately 1700-fold) over PLD2 were developed.
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.[Pubmed:19136975]
Nat Chem Biol. 2009 Feb;5(2):108-17.
Phospholipase D (PLD) is an essential enzyme responsible for the production of the lipid second messenger phosphatidic acid. Phosphatidic acid participates in both G protein-coupled receptor and receptor tyrosine kinase signal transduction networks. The lack of potent and isoform-selective inhibitors has limited progress in defining the cellular roles of PLD. We used a diversity-oriented synthetic approach and developed a library of PLD inhibitors with considerable pharmacological characterization. Here we report the rigorous evaluation of that library, which contains highly potent inhibitors, including the first isoform-selective PLD inhibitors. Specific members of this series inhibit isoforms with >100-fold selectivity both in vitro and in cells. A subset of inhibitors was shown to block invasiveness in metastatic breast cancer models. These findings demonstrate the power of diversity-oriented synthesis combined with biochemical assays and mass spectrometric lipid profiling of cellular responses to develop the first isoform-selective PLD inhibitors--a new class of antimetastatic agents.
