Cat. No. 2559
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluor
Biological ActivityPotent, 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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
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
Find multiple products by catalog number
New Products in this Area
Potent and selective haspin kinase inhibitorUNC 3230
Potent and selective PIP5K1C inhibitor; antinociceptiveBMS 509744
Potent and selective ITK kinase inhibitorWZ 4003
Potent and selective NUAK1/2 inhibitorTC-S 7010
Potent and selective Aurora kinase A inhibitorBryostatin 2
Protein kinase C activatorZLN 024 hydrochloride
Allosteric AMPK activatorTemsirolimus
mTOR inhibitor; antitumorKN 93 phosphate
CaM kinase II inhibitor; water soluble version of KN 93 (Cat. No. 1278).ETP 45835 dihydrochloride
Mnk1 and Mnk2 inhibitorBryostatin 3
Potent protein kinase C activatorGKA 50
Glucokinase activatorMRT 67307 dihydrochloride
Salt inducible kinase (SIK) inhibitorLDN 209929 dihydrochloride
Potent and selective haspin kinase inhibitorRKI 1447 dihydrochloride
Potent and selective ROCK inhibitor; antitumor
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.