S81800 |
IRAK inhibitor 1 |
源葉(MedMol) | ≥98% |
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- 產(chǎn)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.
- 靶點: IC50: 216 nM (IRAK-4), 3.801 μM (JNK-1), >10 μM (JNK-2);IRAK;?JNK
- 體外研究:
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
- 參考文獻:
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
- 保存條件: -20℃
- 配置溶液濃度參考:
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
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系,公式為:
質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)