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.
All Tocris products are intended for laboratory research use only.
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
Selective PFKFB3 inhibitorPD 0332991 isethionate
Potent, selective Cdk4/6 inhibitor; brain penetrantXL 413 hydrochloride
Potent and selective Cdc7 inhibitorC16
PKR inhibitorRp-8-pCPT-cGMPS sodium
PKG inhibitorTC-S 7004
Potent and selective DYRK1A/B inhibitorTAK 960 hydrochloride
Potent and selective PLK1 inhibitorA12B4C3
Potent and selective polynucleotide kinase/phosphatase (PKNP) inhibitorBMS 345541
Selective allosteric inhibitor of IKK; anti-inflammatoryWH-4-023
Potent and selective Lck and Src inhibitor; also inhibits SIKTC-S 7006
Potent and selective Tpl2 (Cot; MAP3K8) inhibitorOXA 06 dihydrochloride
Potent ROCK inhibitorPCI 29732
Potent BTK inhibitorMps1-IN-1 dihydrochloride
Selective monopolar spindle 1 (Mps1) kinase inhibitorCKI 7 dihydrochloride
CK1 inhibitorT 5601640
Selective LIMK2 inhibitor; antitumor3PO
PFKFB3 inhibitor; antiangiogenicCHR 6494 trifluoroacetate
Potent and selective haspin kinase inhibitorUNC 3230
Potent and selective PIP5K1C inhibitor; antinociceptivetrans-ISRIB
Integrated stress response (ISR) inhibitorBMS 509744
Potent and selective ITK inhibitor
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.