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TPCA-1

Cat No. 2559

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Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophene carboxamide

Biological Activity

Potent, selective inhibitor of IκB kinase-2 (IKK-2) (IC₅₀ = 17.9 nM) that displays > 22-fold selectivity over IKK-1 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 localisation. 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 and MSDS.

Resources

Certificate of Analysis / MSDS

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Material Safety Data Sheet: View current batch

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References

Podolin et al (2005) Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkB kinase 2, TPCA-1 (2-[aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation. J.Pharmacol.Exp.Ther. 312 373. Birrell et al (2005) Ik-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma. Am.J.Respir.Crit.Care Med. 172 962. Birrell et al (2006) IkB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic. Mol.Pharmacol. 69 1791.

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Keywords: TPCA-1, Potent, selective, inhibitors, IKK-2, IκB, IkappaB, kinases, Nuclear, Factor, Kappa, B, inhibitors, NF-κB, NF-kappaB, NF-kB, Cytokine, Signaling, Signalling, Transcription, Factors