| Bioactivity | LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC. Target: AntibacterialLED209 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] | ||||||||||||
| Name | LED209 | ||||||||||||
| CAS | 245342-14-7 | ||||||||||||
| Formula | C19H17N3O2S2 | ||||||||||||
| Molar Mass | 383.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Curtis MM, et al. QseC inhibitors as an antivirulence approach for Gram-negative pathogens. MBio. 2014 Nov 11;5(6):e02165. [2]. Harrison CF, et al. Adrenergic antagonists restrict replication of Legionella. Microbiology. 2015 Jul;161(7):1392-406. [3]. Rasko DA, et al. Targeting QseC signaling and virulence for antibiotic development. Science. 2008 Aug 22;321(5892):1078-80. |