Name: IRAK-1-4 Inhibitor I
Price: 260.00 USD

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    IRAK-1/4 Inhibitor I; N-[1-(2-morpholin-4-ylethyl)benzimidazol-2-yl]-3-nitrobenzamide
    
    CAS Number
    
    509093-47-4
    
    Molecular Formula
    
    C20H21N5O4
    
    Molecular Weight
    
    395.41
    
    Appearance
    
    A solid
    
    Purity
    
    98.17%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥19.75 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Pan B, Gao J, et al. "Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice." Int Immunopharmacol. 2020;85:106597. PMID:32422509
    2. Zha C, Zhang W, et al. "Anti-β(2)GPI/β(2)GPI induces neutrophil extracellular traps formation to promote thrombogenesis via the TLR4/MyD88/MAPKs axis activation." Neuropharmacology. 2018 Jun 5;138:140-150. PMID:29883691
    3. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
    4. Chang MC, Chan CP, et al. "Areca nut components stimulate ADAM17, IL-1α, PGE2 and 8-isoprostane production in oral keratinocyte: role of reactive oxygen species,EGF and JAK signaling." Oncotarget. 2016 Mar 29;7(13):16879-94. PMID:26919242

IRAK-1-4 Inhibitor I

IRAK-1-4 Inhibitor I

Background

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