Catalog Number: 2559
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Biological Activity
Potent, selective inhibitor of IκB kinase (IKK) β (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKKα and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localization. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.
Technical Data
  • M.Wt:
    279.29
  • Formula:
    C12H10FN3O2S
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >97%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    507475-17-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and
    Podolin et al.
    J.Pharmacol.Exp.Ther., 2005;312:373
  2. IK-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma.
    Birrell et al.
    Am.J.Respir.Crit.Care Med., 2005;172:962
  3. IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.
    Birrell et al.
    Mol.Pharmacol., 2006;69:1791

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