中文名 | IRAK inhibitor 1 |
英文名 | IRAK inhibitor 1 |
别名 | 环巴胺抑制剂 1 |
英文别名 | 6-imidazo[1 IRAK inhibitor IRAK inhibitor 1 Cyclopamine inhibitor 1 2-a]pyridin-3-yl-N-4-piperidinyl- 6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine 2-PyridinaMine, 6-iMidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl- |
CAS | 1042224-63-4 |
化学式 | C17H19N5 |
分子量 | 293.37 |
密度 | 1.32 |
溶解度 | DMSO: 12.2 mg/mL |
酸度系数 | 9.94±0.10(Predicted) |
存储条件 | -20℃ |
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. |
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 |
5 mM | 0.068 ml | 0.341 ml | 0.682 ml |
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