Cat. No. 3318
Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxa
Biological ActivityOrally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 μM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 μM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.
Licensing InformationSold for research purposes under agreement from AstraZeneca
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
Kishore et al (2003) A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts. J.Biol.Chem. 278 32861. PMID: 12813046.
Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817.
Gomez et al (2005) Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br.J.Pharmacol. 146 217. PMID: 15997236.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: SC 514, supplier, IKK-2, inhibitors, attenuates, NF-κB, NF-kappaB-induced, gene, expression, NF-kB, IKK, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, NF-kappaB, Cytokine, Signaling, Signalling, Transcription, Factors, SC514, AstraZeneca
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
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.