IRAK inhibitor 1

SKU: orb1227075

Description

IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, shows little to no activity against JNK-1 and JNK-2 with IC50 of 3.801 uM and >10 uM, respectively.

Research Area

Immunology & Inflammation; Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1042224-63-4
• MW: 293.37
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₉N₅
• SMILES: C1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4
• Target: IRAK
• Solubility: DMSO: 12.2 mg/mL

Bioactivity

• In Vitro:
  IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme assay but is poorly active against JNK-1 and JNK-2. IRAK-4 is a novel member of the IRAK family with unique functional properties. IRAK-4 is the closest human homolog to Pelle. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner, and overexpression of IRAK-4 can activate NF-κB as well as mitogen-activated protein (MAP) kinase pathways. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its kinase activity to activate NF-κB. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression of dominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting a role of IRAK-4 as a central element in the early signal transduction of Toll/IL-1 receptors, upstream of IRAK-1. IRAK-4 shares the domain structure of the other IRAKs and it is able to activate similar signal transduction pathways, namely NF-κB and MAPK pathways. It rapidly and transiently associates with IRAK-1 and TRAF6 in an IL-1-dependent manner but it is not functionally redundant with IRAK-1. IRAK-4 is an active protein kinase and requires its kinase activity to activate NF-κB. IRAK-4 might act upstream of IRAK-1 as an IRAK-1 activator.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

IRAK