509093-47-4

IRAK-1/4 Inhibitor (interleukin-1 receptor-associated kinases) are important mediators in signal transduction of TIR family members. This regulation protects against the development of cancers and other diseases.

irak-1-4 inhibitor i is an inhibitor of both irak-1 and irak-4 with ic50 values of 0.3μm and 0.2μm , respectively [1].il-1 receptor-associated kinases play important roles in signal transduction. there are totally four members of the iraks, they are irak-1, irak-2, irak-m and irak-4. irak-4 can activate nf-κb and mapk pathways and it is shown that the inhibition of irak-4 can be an anti-inflammatory therapy. irak-1-4 inhibitor i is an analog of an initial irak-4 inhibitor hit, which is screened out from a small molecule li brary against irak-4. with the less basic n-ethylenemorpholine moiety, irak-1-4 inhibitor i has a higher potency than other analogs. additionally, it does not show any cytotoxicity in a 72 h proliferation assay in hela cells(ed50 >30μm) [1].

IRAK1 overexpression leads to the development of head and neck squamous cell carcinoma (HNSCC). Therefore, IRAK-1/4 inhibitor I might be a potential therapeutic for HNSCC tumors. Various experimental studies states that IRAK-1/4 inhibitor might have a potential to exhibit?inhibitory effects on the nuclear factor (NF)-κB signaling pathway.

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[1] jay p. powers, shyun li, juan c. jaen, jinqian liu, nigel p. c. walker, zhulun wang and holger wesche. discovery and initial sar of inhibitors of interleukin-1 receptor-associated kinase-4. bioorganic & medicinal chemistry letters. 2006, 16: 2842–2845.