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509093-47-4

509093-47-4 structure
509093-47-4 structure
  • Name: IRAK-1-4 Inhibitor I
  • Chemical Name: N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide
  • CAS Number: 509093-47-4
  • Molecular Formula: C20H21N5O4
  • Molecular Weight: 395.41200
  • Catalog: Signaling Pathways Immunology/Inflammation IRAK
  • Create Date: 2018-05-05 08:00:00
  • Modify Date: 2024-01-04 11:13:18
  • 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.

Name N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide
Synonyms 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
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
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.

Density 1.4
Molecular Formula C20H21N5O4
Molecular Weight 395.41200
Exact Mass 395.15900
PSA 108.70000
LogP 3.37410
Storage condition 2-8℃
Risk Phrases 25-36/37/38
Safety Phrases 26-36/37-45
RIDADR UN 2811 6.1/PG 3