货号 | 10010267-5mg |
描述 | SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.1,2 In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).1 SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells3 and TLR2 in TNF-activated astrocytes.4 |
供应商 | Cayman |
应用文献 | |
1.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). 2.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). 3.Gomez, A.B.,MacKenzie, C.,Paul, A., et al. Selective inhibition of inhibitory kappa B kinase-b abrogates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. British Journal of Pharmacology 146, 217-225 (2005). 4.Phulwani, N.K.,Esen, N.,Syed, M.M., et al. TLR2 expression in astrocytes is induced by TNF-α-and NF- k B-dependent pathways. Journal of Immunology 181, 3841-3849 (2008). | |
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 | 224.3 |
分子式 | C9H8N2OS2 |
CAS号 | 354812-17-2 |
稳定性 | ≥ 2 years |
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