| 货号 | 11140-1mg |
| 描述 | The NF-κB/Rel family of transcription factors induce and coordinate the expression of pro-inflammatory genes including cytokines, chemokines, interferons, MHC proteins, growth factors, and cell adhesion molecules. Under resting conditions NF-κB dimers are retained in the cytoplasm by a member of the IKB family of inhibitory proteins. Upon activation by cytokines or other stimuli, IKK phosphorylates IKB, initiating a signaling cascade to activate gene transcription.1,2,3 CAY10657 is a thiophenecarboximide derivative proposed to inhibit IKK2.4 Currently, there are no published reports of its biological activity. However, inhibition of NF-κB activation is likely to be of broad utility in the treatment of inflammatory diseases and cancer.5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Delhase, M.,Hayakawa, M.,Chen, Y., et al. Positive and negative regulation of IκB kinase activity through IKKβ subunit phophorylation. Science 284, 309-313 (1999). 2.Israël, A. The IKK complex: an integrator of all signals that activate NF-κB. Trends in Cell Biology 10, 129-133 (2000). 3.Mercurio, F.,Zhu, H.,Murray, B.W., et al. IKK-1 and IKK-2: Cytokine-activated IκB kinases essential for NF-κB activation. Science 278(5339), 860-866 (1997). 4.Faull, A.,Johnstone, C.,Morley, A., et al. Novel compounds. PCT/SE02/01403, 1-175 (2003). 5.Baxter, A.,Brough, S.,Cooper, A., et al. Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorganic & Medicinal Chemistry Letters 14, 2817-2822 (2004). 6.Kishore, N.,Sommers, C.,Mathialagan, S., et al. A selective IKK-2 inhibitor blocks NF- k B-dependent gene expression in interleukin-1ß-stimulated synovial fibroblasts. The Journal of Biological Chemisty 278(35), 32861-32871 (2003). | |
| 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 | 360.4 |
| 分子式 | C17H20N4O3S |
| CAS号 | 494772-86-0 |
| 稳定性 | ≥ 2 years |
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