1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIRAK inhibitor 1Cat. No.: HY-13275CAS No.: 1042224-63-4分式: CHN分量: 293.37作靶點(diǎn): IRAK作通路: Immunology/Inflammation; Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 12.

2、2 mg/mL (41.59 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.4087 mL 17.0433 mL 34.0866 mL5 mM 0.6817 mL 3.4087 mL 6.8173 mL10 mM 0.3409 mL 1.7043 mL 3.4087 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 IRAK inhibitor 1種有效的 IRAK-4 抑制劑，IC5

3、0 為 216 nM，微弱抑制 JNK-1 和 JNK-2，IC50 分別為3.801 M 和 10 M。IC50 & Target IC50: 216 nM (IRAK-4), 3.801 M (JNK-1), 10 M (JNK-2) 1體外研究IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme assay but is poorly active against JNK-1and JNK-2 1. IRAK-4 is a novel member of the IRAK family with unique

4、 functional properties. IRAK-4 is the1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEclosest 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-B as well as mitogen-activated protein(MAP) kinase pathway

5、s. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its kinaseactivity to activate NF-B. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression ofdominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting arole of IR

6、AK-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 transductionpathways, namely NF-B and MAPK pathways. It rapidly and transiently associates with IRAK-

7、1 and TRAF6in an IL-1-dependent manner but it is not functionally redundant with IRAK-1. IRAK-4 is an active proteinkinase and requires its kinase activity to activate NF-B. IRAK-4 might act upstream of IRAK-1 as an IRAK-1activator 2.REFERENCES1. Buckley GM, et al. IRAK-4 inhibitors. Part II: A stru

8、cture-based assessment of imidazo1,2-apyridine 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 Apr16;99(8):5567-72.McePdfHeightCaution: Product has not been fully validated for medical applications.F