| LED209Highly selective for histidine sensor kinase QseC |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.08%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
LED209 Dilution Calculator
calculate
LED209 Molarity Calculator
calculate
| Cas No. | 245342-14-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | N-phenyl-4-(3-phenylthioureido)benzenesulfonamide | ||
| Canonical SMILES | O=S(C1=CC=C(NC(NC2=CC=CC=C2)=S)C=C1)(NC3=CC=CC=C3)=O | ||
| Formula | C19H17N3O2S2 | M.Wt | 383.49 |
| Solubility | ＜3.83 mg/mL in DMSO, <2.33 mg/ml="" in="" etoh,=""><2.38 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
Description:
IC50: <10>
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.
