Home » Pharmacology » Enzymes » Kinases » IκB Kinase » TPCA-1

TPCA-1

Cat. No. 2559

Price and Availability

For TPCA-1 pricing & availability please select your country from the drop down menu:
Submit

By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Select another batch:

Safety Data Sheet: View Safety Data Sheet

References

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. PMID: 16002568.

Podolin et al (2005) 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 antigen-induced T cell proliferation. J.Pharmacol.Exp.Ther. 312 373. PMID: 15316093.

Birrell et al (2006) IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic. Mol.Pharmacol. 69 1791. PMID: 16517756.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Cytokine and NF-κB Signaling IκB Kinase Kinases

NF-κB & IκB Transcription Factors

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