| 货号 | 16667-1mg |
| 描述 | BMS 345541 is a cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50s = 4 and 0.3 µM).1 It is without effect against a panel of other serine/threonine and tyrosine kinases at 100 µM.1 BMS 345541 inhibits signaling through nuclear factor-κB (NF-κB) both in cells and in vivo, showing excellent pharmacokinetics in mice.1 It blocks joint inflammation and damage in collagen-induced arthritis in mice and induces apoptosis in melanoma cells both in vitroandin vivo.2,3 BMS 345541 is used to explore novel roles for IKK phosphorylation and NF-κB signaling.4,5 |
| 别名 | IKK Inhibitor III; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Burke, J.R.,Pattoli, M.A.,Gregor, K.R., et al. 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. The Journal of Biological Chemisty 278(3), 1450-1456 (2003). 2.McIntyre, K.W.,Shuster, D.J.,Gillooly, K.M., et al. A highly selective inhibitor of IκB kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice. Arthritis and Rheumatism 48(9), 2652-2659 (2003). 3.Yang, J.,Amiri, K.I.,Burke, J.R., et al. BMS-345541 targets inhibitor of κB kinase and induces apoptosis in melanoma: Involvement of nuclear factor κB and mitochondria pathways. Clinical Cancer Research 12(3 Pt 1), 950-960 (2006). 4.Karim, Z.A.,Zhang, J.,Bangerjee, M., et al. IκB kinase phosphorylation of SNAP-23 controls platelet secretion. Blood 121(22), 4567-4574 (2013). 5.Wen, L.,Zhu, M.,Madigan, M.C., et al. Immunomodulatory effects of bone marrow-derived mesenchymal stem cells on pro-inflammatory cytokine-stimulated human corneal epithelial cells. PLoS One 9(7), 1-12 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 483.4 |
| 分子式 | C14H17N5 • 2CF3COOH |
| 稳定性 | ≥ 2 years |
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