IRAK-1/4 Inhibitor

Interleukin-1 receptor-associated kinases (IRAKs) are important mediators in the signal transduction of Toll/IL-1 receptor (TIR) family members. Dysregulation of TIR signaling, typified by increased NF-kappaB activity, results in the development of some cancers and other diseases, making the development of IRAK inhibitors a potential therapeutic strategy. IRAK-1/4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 0.3 and 0.2 µM, respectively. It demonstrates IC50 values >10 µM in a panel of 27 other kinases tested. This compound has been used to inhibit a pro-inflammatory response in microglia isolated from clinically diagnosed Alzheimer's disease patients.Formal Name: N-[1-[2-(4-morpholinyl)ethyl]-1H-benzimidazol-2-yl]-3-nitro-benzamide. CAS Number: 509093-47-4. Molecular Formula: C20H21N5O4. Formula Weight: 395.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.5 mg/ml, DMSO: 1 mg/ml. lambdamax: 224, 259, 322 nm. SMILES: O=C(C1=CC([N+]([O-])=O)=CC=C1)NC2=NC3=CC=CC=C3N2CCN4CCOCC4. InChi Code: InChI=1S/C20H21N5O4/c26-19(15-4-3-5-16(14-15)25(27)28)22-20-21-17-6-1-2-7-18(17)24(20)9-8-23-10-12-29-13-11-23/h1-7,14H,8-13H2,(H,21,22,26). InChi Key: QTCFYQHZJIIHBS-UHFFFAOYSA-N.