TPCA-1 (2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide) | 507475-17-4

name

tpca-1

chemical name

2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

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.

MW

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

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.