| 产品描述: | IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively. |
| 靶点: |
IC50: 216 nM (IRAK-4), 3.801 μM (JNK-1), >10 μM (JNK-2);IRAK; JNK |
| 体外研究: |
IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme assay but is poorly active against JNK-1 and JNK-2. IRAK-4 is a novel member of the IRAK family with unique functional properties. IRAK-4 is the closest human homolog to Pelle. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner, and overexpression of IRAK-4 can activate NF-κB as well as mitogen-activated protein (MAP) kinase pathways. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its kinase activity to activate NF-κB. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression of dominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting a role of IRAK-4 as a central element in the early signal transduction of Toll/IL-1 receptors, upstream of IRAK-1. IRAK-4 shares the domain structure of the other IRAKs and it is able to activate similar signal transduction pathways, namely NF-κB and MAPK pathways. It rapidly and transiently associates with IRAK-1 and TRAF6 in an IL-1-dependent manner but it is not functionally redundant with IRAK-1. IRAK-4 is an active protein kinase and requires its kinase activity to activate NF-κB. IRAK-4 might act upstream of IRAK-1 as an IRAK-1 activator |
| 参考文献: |
1. Buckley GM, et al. IRAK-4 inhibitors. Part II: A structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3291-5. 2. Li S, et al. IRAK-4: a novel member of the IRAK family with the properties of an IRAK-kinase. Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):5567-72. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.409 ml |
17.044 ml |
34.087 ml |
| 5 mM |
0.682 ml |
3.409 ml |
6.817 ml |
| 10 mM |
0.341 ml |
1.704 ml |
3.409 ml |
| 50 mM |
0.068 ml |
0.341 ml |
0.682 ml |
|
| 注意: |
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