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

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Name:IRAK-1-4 Inhibitor I; IRAK-1/4 Inhibitor I
Cat. No. :CS-0704
CAS No. :509093-47-4
Formula:C20H21N5O4
M. Wt. : 395.41
Solubility:10 mM in DMSO

IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1 with IC50 of 0.2 μM and 0.3 μM, respectively.IC50 & 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].

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. 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.