货号 | 5134/10 |
别名 | N-[3-[[5-Cyclopropyl-2-[[3-(4-morph |
供应商 | Tocris |
生物活性 | Salt inducible kinase (SIK) inhibitor (IC50 values are 67, 250 and 430 nM for SIK2, SIK1 and SIK3 respectively). Also inhibits TBK1, MARK1-4, IKKε and NUAK1 (IC50 values are 19, 27-52, 160 and 230 nM respectively). Has no effect on IKKα or IKKβ. Induces IL-10 secretion and inhibits TNF-α and IL-6 secretion in bacterial LPS-stimulated macrophages. Also enhances IL-1-induced activation of NFκB-dependent gene transcription in mouse embryonic fibroblast (MEF) cells. |
运输条件 | Ambient |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 537.52 |
分子式 | C26H36N6O2 |
可溶性/溶解性 | Soluble to 20 mM in water and to 100 mM in DMSO |
参考文献 | Clarket al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986. PMID: 23033494. Clarket al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93. PMID: 21138416. Smithet al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537. PMID: 21204785. |