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
Salt inducible kinase (SIK) inhibitorLDN 209929 dihydrochloride
Potent and selective haspin kinase inhibitorRKI 1447 dihydrochloride
Potent and selective ROCK inhibitor; antitumorLIMKi 3
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 activator
November 15 - 19, 2014
Washington D.C., USA