LED209Highly selective for histidine sensor kinase QseC CAS# 245342-14-7 |
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Quality Control & MSDS
3D structure
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| Cas No. | 245342-14-7 | SDF | Download SDF |
| PubChem ID | 3421033 | Appearance | Powder |
| Formula | C19H17N3O2S2 | M.Wt | 383.49 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : < 1 mg/mL (insoluble or slightly soluble) | ||
| Chemical Name | 1-phenyl-3-[4-(phenylsulfamoyl)phenyl]thiourea | ||
| SMILES | C1=CC=C(C=C1)NC(=S)NC2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=C3 | ||
| Standard InChIKey | HNDRSTUKPCLQLT-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H17N3O2S2/c23-26(24,22-17-9-5-2-6-10-17)18-13-11-16(12-14-18)21-19(25)20-15-7-3-1-4-8-15/h1-14,22H,(H2,20,21,25) | ||
| 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 | LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
Target: Antibacterial
LED209 has desirable pharmacokinetics and does not present toxicity in vitro and in rodents. This is a unique antivirulence approach, with a proven broad-spectrum activity against multiple Gram-negative pathogens that cause mammalian infections.The LED209 QseC inhibitor has a unique mode of action by acting as a prodrug scaffold to deliver a warhead that allosterically modifies QseC, impeding virulence in several Gram-negative pathogens.[1] LED209 is QseC sensor kinase inhibitor , as a potential lead compound to combat infections with Legionella or Mycobacterium spp. [2] LED209 inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 inhibits EHEC virulence traits in vitro. LED209 markedly inhibits the virulence of several pathogens in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs. [3] References: | |||||
LED209 Dilution Calculator
LED209 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | 52.1526 mL | 65.1907 mL |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | 10.4305 mL | 13.0381 mL |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL | 5.2153 mL | 6.5191 mL |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5215 mL | 1.0431 mL | 1.3038 mL |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.5215 mL | 0.6519 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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Description:
IC50: <10 μM
Many bacterial pathogens rely on a conserved membrane histidine sensor kinase, QseC, to respond to host adrenergic signaling molecules and bacterial signals in order to promote the expression of virulence factors. LED209 is a potent prodrug that is highly selective for QseC.
In vitro: LED209-mediated inhibition of virulence gene expression inhibited the secretion of EspA and EspB, two proteins encoded within the locus of enterocyte effacement that are required for Escherichia coli (EHEC) to translocate bacterial proteins into host cells and cause attaching-effacing (AE) lesions. At 5 pM, LED209 abolished EHEC AE lesion formation on cultured epithelial cells. Unlike conventional antibiotics, LED209 does not kill or hinder EHEC growth or trigger the EHEC SOS response [1].
In vivo: LED209 [20 mg per kilogram of body weight (mg/kg)] was given orally to mice 3 hours before and 3 hours after intraperitoneal injection of a lethal dose of S. typhimurium. Twenty-four hours after infection, only 30% of untreated mice remained alive, whereas 80% of the LED209-treated mice were still alive. All the S. typhimurium– infected mice died within 72 hours of infection, and 20% of LED209-treated mice survived up to 12 days [1].
Clinical trial: Up to now, LED209 is still in the preclinical development stage.
Reference:
[1] Rasko DA, Moreira CG, Li de R, Reading NC, Ritchie JM, Waldor MK, Williams N, Taussig R, Wei S, Roth M, Hughes DT, Huntley JF, Fina MW, Falck JR, Sperandio V. Targeting QseC signaling and virulence for antibiotic development. Science. 2008 Aug 22;321(5892):1078-80.
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A potent and selective antimicrobial poly(amidoamine) dendrimer conjugate with LED209 targeting QseC receptor to inhibit the virulence genes of gram negative bacteria.[Pubmed:25461286]
Nanomedicine. 2015 Feb;11(2):329-39.
UNLABELLED: The pandemic of multidrug-resistant Gram negative bacteria (GNB) is a worldwide healthcare concern, and very few antibiotics are being explored to match the clinical challenge. Recently, amino-terminated poly(amidoamine) (PAMAM) dendrimers have shown potential to function as broad antimicrobial agents. However, PAMAM displays a generation dependent cytotoxicity to mammalian cells and low selectivity on bacterial cells, which limits PAMAM to be developed as an antibacterial agent for systemic administration. We conjugated G3 PAMAM with LED209, a specific inhibitor of quorum sensor QseC of GNB, to generate a multifunctional agent PAMAM-LED209. Intriguingly, PAMAM-LED209 showed higher selectivity on GNB and lower cytotoxicity to mammalian cells, yet remained strong antibacterial activity. PAMAM-LED209 also inhibited virulence gene expression of GNB, and did not induce antibiotic-resistance. The present work firstly demonstrated that PAMAM-LED209 conjugate had a highly selective anti-GNB activity and low cytotoxicity, which offered a feasible strategy for combating multidrug-resistant GNB infections. FROM THE CLINICAL EDITOR: This research team demonstrated that a novel PAMAM-LED209 conjugate had highly selective activity against Gram-negative bacteria, coupled with low cytotoxicity, offering a potential strategy for combating multidrug-resistant infections.
