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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
2 mg | $50 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $112 | In Stock | |
25 mg | $258 | In Stock | |
50 mg | $486 | In Stock | |
100 mg | $695 | In Stock | |
500 mg | $1,490 | In Stock | |
1 mL x 10 mM (in DMSO) | $72 | In Stock |
Description | IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1. |
In vitro | IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 μM) against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60SRC. Additionally, IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 μM)[1]. IRAK-1/4 inhibitor eliminates the LPS-induced increases in Bcl10, NF-κB, 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 5.18±0.22 to 2.36±0.08 ng/mL), and the IL-8 response decline by 60% (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]. |
Alias | IRAK-1/4 Inhibitor I, IRAK-1/4 Inhibitor |
Molecular Weight | 395.41 |
Formula | C20H21N5O4 |
Cas No. | 509093-47-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||
Solubility Information | DMSO: 8.13 mg/mL (20.55 mM) ![]() | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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