IRAK-1-4-Inhibitor-I-IRAK-1-4-Inhibitor-I-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIRAK-1-4 Inhibitor ICat. No.: HY-13329CAS No.: 509093-47-4Synonyms: IRAK-1/4 Inhibitor I分式: CHNO分量: 395.41作靶点: IRAK作通路: Immunology/Inflammation; Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mont

2、hs-20C 1 month溶解性数据体外实验 DMSO : 14.29 mg/mL (36.14 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5290 mL 12.6451 mL 25.2902 mL5 mM 0.5058 mL 2.5290 mL 5.0580 mL10 mM 0.2529 mL 1.2645 mL 2.5290 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄

3、清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.43 mg/mL (3.62 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 IRAK-1-4 I

4、nhibitor I是IRAK1/4 抑制剂，IC50 分别为 0.2 M 和 0.3 M。IC50 & Target IC50: 0.2 M (IRAK-4), 0.3 M (IRAK-1) 1体外研究 IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 M) against a panel of 27 otherkinases, including the most closely homologous (outside of the IRAK family) Lck and pp6

5、0SRC. Additionally,IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells(ED5030 M). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 M) 1.IRAK-1/4 inhibitor eliminates the LPS-induced increases in Bcl10, NF-B,

6、and IL-8. IRAK-1/4 mediates LPS-induced IL-8 activation and functions upstream of Bcl10. The LPS-induced increase in Bcl10 declines by 73%(from 5.180.22 to 2.360.08 ng/mL), and the IL-8 response decline by 60% (from 2.640.31 to 1.140.08ng/mL) 2.PROTOCOLCell Assay 2 NCM460 cells, grown in 24-well pla

7、tes, are incubated with 50 M IRAK-1/4 inhibitor for 2 h. After 2 h, themedia are changed, and new media with or without LPS (10 ng/mL) added. Treatment is terminated at 6 h,and spent media and cells are collected for IL-8 and other assays 2.MCE has not independently confirmed the accuracy of these m

8、ethods. They are for reference only.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Sci Rep. 2016 Jun 8;6:27460.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Powers JP, et al. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-

9、4. Bioorg Med Chem Lett. 2006 Jun1;16(11):2842-2845.2. Bhattacharyya S, et al. Bcl10 mediates LPS-induced activation of NF-kappaB and IL-8 in human intestinal epithelial cells. Am J PhysiolGastrointest Liver Physiol. 2007 Aug;293(2):G429-37.McePdfHeightCaution: Product has not been fully validated for medical