Name | IRAK-1-4 Inhibitor I |
Description | IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4. |
Cell Research | IRAK-1-4 Inhibitor I is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. NCM460 cells, grown in 24-well plates, are incubated with 50 μM IRAK-1/4 inhibitor for 2 h. After 2 h, the media 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]. |
Kinase Assay | Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1. |
In vitro | IRAK-1-4 Inhibitor I exhibits an IC50 greater than 10 μM against a panel of 27 kinases, including homologous kinases Lck and pp60SRC. It shows no cytotoxicity in a 72-hour proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is achieved with an IC50 of 0.3 μM[1]. IRAK-1/4 Inhibitor eliminates LPS-induced increases in Bcl10, NF-κB, and IL-8, with a 73% reduction in Bcl10 (from 5.18±0.22 to 2.36±0.08 ng/mL) and a 60% reduction in IL-8 (from 2.64±0.31 to 1.14±0.08 ng/mL)[2]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 8.13 mg/mL (20.55 mM), Sonication is recommended.
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Keywords | IRAK | inhibit | IRAK-1-4 Inhibitor I | Interleukin-1 receptor associated kinase | IRAK 1 4 Inhibitor I | IRAK14 Inhibitor I | IL-1R associated kinase | Inhibitor |
Inhibitors Related | IRAK inhibitor 2 | IRAK inhibitor 1 | IRAK4-IN-1 | IRAK-4 protein kinase inhibitor 2 | ANTHRAQUINONE-2-CARBOXYLIC ACID | Thalidomide 4-fluoride | IRAK4-IN-20 | GLPG2534 | Zabedosertib | Zimlovisertib | AS-2444697 | JH-X-119-01 |
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