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IRAK-1-4 Inhibitor I

IRAK-1-4 Inhibitor I 是一种IRAK1/4双重抑制剂，其IC50分别为 0.2 μM 和 0.3 μM。

CAS号

509093-47-4

分子式

C20H21N5O4

主要靶点

IRAK

仅限科研使用

Cat No : CM04856

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Synonyms

IRAK-1/4 Inhibitor|IRAK-1/4 Inhibitor I

验证数据展示

  • CAS No.: 509093-47-4

    IRAK-1-4 Inhibitor I
    CAS#: 509093-47-4

产品信息

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

CAS号 509093-47-4
分子式 C20H21N5O4
主要靶点 IRAK
主要通路 免疫与炎症|NF-κB信号通路
分子量 395.41
纯度 100.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 IRAK-1/4 Inhibitor|IRAK-1/4 Inhibitor I

靶点活性

IRAK 4:0.3 μM|IRAK 1:0.2 μM

体外活性

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].

溶解度

DMSO:7.9 mg/mL(20 mM)

细胞实验

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].

参考文献

1.Powers JP, et al. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorg Med Chem Lett. 2006 Jun 1;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 Physiol Gastrointest Liver Physiol. 2007 Aug;293(2):G429-37.
3.Wu X, Xu M, Liu Y, et al. Dual Pharmacological Inhibition of IRAK1 and IRAK4 Prevents LPS Induced Monocyte Adhesion to Endothelial Cells[J]. bioRxiv. 2021

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The dilution calculator equation

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