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IRAK-1-4 Inhibitor I

Names

[ CAS No. ]:
509093-47-4

[ Name ]:
IRAK-1-4 Inhibitor I

[Synonym ]:
Benzamide,N-[1-[2-(4-morpholinyl)ethyl]-1H-benzimidazol-2-yl]-3-nitro
IRAK-1/4 Inhibitor
N-(2-Morpholinylethyl)-2-(3-nitrobenzoylamido)-benzimidazole
Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor
IRAK-1/4 Inhibitor I
IRAK-1-4 Inhibitor I

Biological Activity

[Description]:

IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> IRAK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK
Research Areas >> Inflammation/Immunology

[Target]

IC50: 0.2 μM (IRAK-4), 0.3 μM (IRAK-1)[1]


[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].

[Cell Assay]

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].

[References]

[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.


[Related Small Molecules]

PF06650833 | CA-4948 | ginsenoside Rb1 | IRAK4-IN-1 | IRAK inhibitor 1 | IRAK inhibitor 4 | IRAK inhibitor 2 | IRAK inhibitor 3 | IRAK inhibitor 6

Chemical & Physical Properties

[ Density]:
1.4

[ Molecular Formula ]:
C20H21N5O4

[ Molecular Weight ]:
395.41200

[ Exact Mass ]:
395.15900

[ PSA ]:
108.70000

[ LogP ]:
3.37410

[ Storage condition ]:
2-8℃

Safety Information

[ Risk Phrases ]:
25-36/37/38

[ Safety Phrases ]:
26-36/37-45

[ RIDADR ]:
UN 2811 6.1/PG 3

Related Compounds