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
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 inhibitorTC-S 7003
Potent Lck inhibitorML 281
STK33 inhibitorCRT 0066101
Potent protein kinase D (PKD) inhibitorHarmine
Potent and selective Dyrk1A inhibitorAZ 628
Potent Raf kinase inhibitorCHIR 99021 trihydrochloride
Hydrochloride salt of CHIR 99021 (Cat. No. 4423); selective GSK-3 inhibitorYZ9
PFKFB3 inhibitor; inhibits cell growthKU 0060648
Dual DNA-PK and PI 3-K inhibitorKB SRC 4
Potent and selective c-Src inhibitor
Meet your representative
July 15, 2014