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 LIM kinase inhibitor; antitumorFRAX 486
Potent p21-activated kinase (PAK) inhibitor; brain penetrant and orally bioavailableBIX 02189
Selective MEK5 and ERK5 inhibitorTC Mps1 12
Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor; orally activeGSK 2606414
Potent and selective PERK inhibitor; orally bioavailableAZ 20
Potent and selective ATR kinase inhibitor; antitumorAZD 7762 hydrochloride
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2PHT 427
Dual Akt and PDK1 inhibitor; antitumorML 786 dihydrochloride
Potent Raf kinase inhibitor; orally bioavailableSenexin A
Cyclin-dependent kinase 8 (cdk8) inhibitorXL 388
Potent and selective mTOR inhibitor; antitumorPS 1145 dihydrochloride
Selective IKK inhibitor; orally activeRSVA 405
AMPK activatorAtiprimod dihydrochloride
JAK2 inhibitorAIM 100
Potent and selective Ack1 inhibitorML 120B dihydrochloride
Novel IKK2-selective inhibitorML 202
Pyruvate kinase M2 activatorGNF 5
Selective allosteric inhibitor of Bcr-Abl; analog of GNF 2 (Cat. No. 4399)TC-S 7005
Potent and selective PLK2 inhibitorSRPIN340
Selective SRPK1 inhibitor
July 23 - 27, 2014
Bonn University, Germany