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]. The IRAK-1/4 inhibitor suppresses LPS-induced elevations in Bcl10, NF-κB, and IL-8. It mediates the LPS-induced activation of IL-8 and operates upstream of Bcl10. Following treatment, Bcl10 levels decrease by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and IL-8 levels drop by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL)[2].
体外研究
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].
The IRAK-1/4 inhibitor suppresses LPS-induced elevations in Bcl10, NF-κB, and IL-8. It mediates the LPS-induced activation of IL-8 and operates upstream of Bcl10. Following treatment, Bcl10 levels decrease by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and IL-8 levels drop by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL)[2].
作用机制
IRAK-1-4 Inhibitor I plays the role of IRAK-4 inhibitor by binding with acyl-2-aminobenzimidazole scaffold that represents a unique kinase binding motif.
Tags:
IRAK-1-4 Inhibitor I | 509093-47-4 | IRAK-1/4 Inhibitor I | IRAK | IRAK Inhibitor | Immunology/Inflammation | IRAK | 仅供科研使用 | AmBeed-信号通路专用抑制剂
| IRAK-1-4 Inhibitor I 纯度/质量文件
| IRAK-1-4 Inhibitor I 生物活性
| IRAK-1-4 Inhibitor I 动物研究
| IRAK-1-4 Inhibitor I 参考文献
| IRAK-1-4 Inhibitor I 实验方案
| IRAK-1-4 Inhibitor I 技术信息
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