IRAK-1/4 Inhibitor

Cas No.:	509093-47-4
Chemical Name:	IRAK-1/4 INHIBITOR I
Synonyms:	IRAK-1-4 Inhibitor I;N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide;β-Asarone NEW;4 Inhibitor;4 INHIBITOR I;AGN-PC-00J89M;Benzamide, N-[1-[2-(4-morpholinyl)ethyl]-1H-benzimidazol-2-yl]-3-nitro-;CHEMBL379787;Interleukin-1 Receptor-Associated-Kinase-1;IRAK-1;N-(2-Morpholinylethyl)-2-(3-nitrobenzoylamido)-benzimidazole;SureCN3600534;3-Nitro-N-(1-(2-morpholin-4-ylethyl)-1H-benzimidazol-2-yl)benzamide;IRAK-1/4 INHIBITOR I
SMILES:	O=C(C1=CC=CC([N+]([O-])=O)=C1)NC2=NC3=CC=CC=C3N2CCN4CCOCC4
Formula:	C20H21N5O4
M.Wt:	395.41184
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.

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].