货号 | 4806/50 |
别名 | N1-(1,8-Dimethylimidazo[1,2-a]quino |
供应商 | Tocris |
生物活性 | Selective allosteric inhibitor of IKK (IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively). Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. Also suppresses joint destruction in a mouse model of arthritis. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >99 % |
计算分子量 | 291.78 |
分子式 | C14H17N5.HCl |
可溶性/溶解性 | Soluble to 100 mM in water and to 100 mM in DMSO |
参考文献 | De Silvaet al (2010) Inhibition of choriodecidual cytokine production and inflammatory gene expression by selective IκB kinase (IKK) inhibitors. Br.J.Pharmacol. 160 1808. PMID: 20649582. Pattoliet al (2005) Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression. J.Pharmacol.Exp.Ther. 315 382. PMID: 16009742. Burkeet al (2003) BMS-345541 is a highly selective inhibitor of IκB kinase that binds at an allosteric site of the enzyme and blocks NF- κB-dependent transcription in mice. J.Biol.Chem. 278 1450. PMID: 12403772. |