LED209 - CAS 245342-14-7
Catalog number: 245342-14-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
LED209 is a highly selective for histidine sensor kinase QseC that blocks both norepinephrine- and epinephrine-triggered QseC-dependent virulence gene expression at 5 pM in vitro.
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White powder
1-phenyl-3-[4-(phenylsulfamoyl)phenyl]thiourea LED209 245342-14-7 LED-209 HNDRSTUKPCLQLT-UHFFFAOYSA-N N-Phenyl-4-(3-phenylthioureido)benzenesulfonamide N-phenyl-4-[[(phenylamino)thioxomethyl]amino]benzenesulfonamide AC1MQ46P CHEMBL516533 SCHEMBL3396831
Soluble to < 3.8 mg/mL in DMSO
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -117℃ for long term (months to years).
Shelf Life:
2 years
Boiling Point:
549.4±60.0 °C | Condition: Press: 760 Torr
1.437±0.06 g/cm3
Canonical SMILES:
1.QseC inhibitors as an antivirulence approach for Gram-negative pathogens.
Curtis MM, Russell R, Moreira CG, Adebesin AM, Wang C1, Williams NS1, Taussig R2, Stewart D3, Zimmern P4, Lu B, Prasad RN, Zhu C, Rasko DA5, Huntley JF6, Falck JR, Sperandio V7. MBio. 2014 Nov 11;5(6):e02165. doi: 10.1128/mBio.02165-14.
Invasive pathogens interface with the host and its resident microbiota through interkingdom signaling. The bacterial receptor QseC, which is a membrane-bound histidine sensor kinase, responds to the host stress hormones epinephrine and norepinephrine and the bacterial signal AI-3, integrating interkingdom signaling at the biochemical level. Importantly, the QseC signaling cascade is exploited by many bacterial pathogens to promote virulence. Here, we translated this basic science information into development of a potent small molecule inhibitor of QseC, LED209. Extensive structure activity relationship (SAR) studies revealed that LED209 is a potent prodrug that is highly selective for QseC. Its warhead allosterically modifies lysines in QseC, impairing its function and preventing the activation of the virulence program of several Gram-negative pathogens both in vitro and during murine infection. LED209 does not interfere with pathogen growth, possibly leading to a milder evolutionary pressure toward drug resistance.
2.A potent and selective antimicrobial poly(amidoamine) dendrimer conjugate with LED209 targeting QseC receptor to inhibit the virulence genes of gram negative bacteria.
Xue XY1, Mao XG2, Li Z1, Chen Z1, Zhou Y1, Hou Z1, Li MK1, Meng JR1, Luo XX3. Nanomedicine. 2015 Feb;11(2):329-39. doi: 10.1016/j.nano.2014.09.016. Epub 2014 Nov 15.
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.
3.Targeting QseC signaling and virulence for antibiotic development.
Rasko DA1, 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. Science. 2008 Aug 22;321(5892):1078-80. doi: 10.1126/science.1160354.
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. Using a high-throughput screen, we identified a small molecule, LED209, that inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 is not toxic and does not inhibit pathogen growth; however, this compound markedly inhibits the virulence of several pathogens in vitro and in vivo in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs.
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CAS 245342-14-7 LED209

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