IRAK-1/4 Inhibitor

• CAT Number: I003813
• CAS Number: 509093-47-4
• Molecular Formula: C₂₀H₂₁N₅O
• Molecular Weight: 395.41
• Purity: ≥95%
• Synonyms: IRAK-1/4 Inhibitor I; Benzamide, N-[1-[2-(4-morpholinyl)ethyl]-1H-benzimidazol-2-yl]-3-nitro-
• Target: IRAK
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 200 nM
• InChI: 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)
• InChIKey: QTCFYQHZJIIHBS-UHFFFAOYSA-N
• SMILES: C1COCCN1CCN2C3=CC=CC=C3N=C2NC(=O)C4=CC(=CC=C4)[N+](=O)[O-]

IRAK-1-4 Inhibitor I(cas 509093-47-4) is an inhibitor of interleukin-1 receptor associated kinase (IRAK) with IC₅₀ values of 0.3 μM and 0.2 μM for IRAK-1 and IRAK-4, respectively. It displays IC₅₀ values >10 μM in a panel of 27 other kinases tested.

Reference

1. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2842-5. Epub 2006 Mar 24.
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated
kinase-4.
Powers JP(1), Li S, Jaen JC, Liu J, Walker NP, Wang Z, Wesche H.
Author information:
(1)Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

High-throughput screening of a small-molecule compound library resulted in the
identification of a novel series of N-acyl 2-aminobenzimidazoles that are potent
inhibitors of interleukin-1 receptor-associated kinase-4.