| 货号 | 3318/50 |
| 别名 | 4-Amino-[2',3'-bithiophene]-5-carboxa |
| 供应商 | Tocris |
| 生物活性 | Orally 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. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 224.3 |
| 分子式 | C9H8N2OS2 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in ethanol |
| CAS号 | 354812-17-2 |
| 参考文献 | Gomezet 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. Baxteret al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 142817. Kishoreet 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. |