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IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $37 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $112 | In Stock | In Stock | |
| 25 mg | $235 | In Stock | In Stock | |
| 50 mg | $396 | In Stock | In Stock | |
| 100 mg | $569 | In Stock | In Stock | |
| 500 mg | $1,190 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $72 | In Stock | In Stock |
| Description | IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4. |
| Targets&IC50 | IRAK1:0.2 μM, IRAK4:0.3 μM |
| 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]. |
| 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. |
| 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]. |
| Synonyms | IRAK-1/4 Inhibitor I, IRAK-1/4 Inhibitor |
| Molecular Weight | 395.41 |
| Formula | C20H21N5O4 |
| Cas No. | 509093-47-4 |
| Smiles | [O-][N+](=O)c1cccc(c1)C(=O)Nc1nc2ccccc2n1CCN1CCOCC1 |
| Relative Density. | 1.40 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 7.88 mg/mL (19.93 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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