Name: IRAK inhibitor 6
Price: 436.00 USD

- Overview
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    Background
    
    IC50: 0.16 μM for IRAK-4 IRAK inhibitor 6 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.The interleukin-1 receptor associated kinases (IRAKs) are a family of serine/threonine kinases related with regulating cellular signalling downstream of the IL-18, IL-1 and various Toll-like receptors. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NFКB and MAPK pathways, which are critical for the production of inflammatory cytokines.In vitro: A quantitative structure–activity relationship (QSAR) study of IRAK inhibitor 6 and its analogs were conducted by using the genetic algorithm and multiple linear regression (GA-MLR) method [1]. In vitro study showed that compared with its unsubstituted phenyl amide analog, the ortho-substitution with chloro, methoxy and difluoromethoxy analogs of IRAK inhibitor 6 improved potency against IRAK-4 significantly. These potency effects were additive, with the most active example in the set being IRAK inhibitor 6, in which the presence of nitrogen-linked substituents at the para position had a beneficial effect on the rate of turnover by human microsomes (20 μL/min/mg protein) [2]. Clinical trial: N/A
    
    [1] Pourbasheer E, Riahi S, Ganjali MR, Norouzi P. Quantitative structure-activity relationship (QSAR) study of interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor activity by the genetic algorithm and multiple linear regression (GA-MLR) method. J Enzyme Inhib Med Chem. 2010 Dec;25(6):844-53.
    [2] Buckley GM, Gowers L, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V, Fraser JL. IRAK-4 inhibitors. Part 1: a series of amides. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3211-4.
- Properties
  - Alternative Name
    
    N-(2-methoxy-4-morpholin-4-ylphenyl)-2-pyridin-3-yl-1,3-thiazole-4-carboxamide
    
    CAS Number
    
    1042672-97-8
    
    Molecular Formula
    
    C20H20N4O3S
    
    Molecular Weight
    
    396.46
    
    Appearance
    
    A solid
    
    Purity
    
    98.77%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥9.9 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

IRAK inhibitor 6

IRAK inhibitor 6

Background

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