Name: IKK-16 (hydrochloride)
Price: 244.00 USD

- Overview
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    Background
    
    IC50: 200, 40, and 70 nM for IKKα, IKKβ, and IKK complex, respectively.IKK-16 is an IκB kinases (IKKs) inhibitor.The IκB kinase (IKK), part of a high molecular weight protein complex consisting of three subunits, IKK1, IKK2, and IKKc, emerged as a prime target for the development of novel anti-rheumatic and anti-inflammatory drugs.In vitro: In screening study, it was found that compounds with an additional basic amino group were more active than the neutral inhibitors. The tertiary amines, such as IKK-16, was active in the low-nanomolar range. IKK-16 could inhibit TNFa-induced adhesion molecule expression in a potency range similar to the IjBa degradation. Although IKK-16 showed activity in the IFNc-induced expression of b2 microglobulin, its potency was weaker. These data demonstrated that IKK-16 had an effect on downstream gene expression, however, on the cellular level the selectivity was modest [1].In vivo: Animal study found that the treatment with IKK 16 to mice could attenuate the impairment in systolic contractility, renal dysfunction, hepatocellular injury and lung inflammation in LPS/PepG-induced MOD and in polymicrobial sepsis. IKK-16 treatment could also significantly attenuated the increase in inducible nitric oxide synthase (iNOS) expression and increase the phosphorylation of Akt and endothelial nitric oxide synthase [2].Clinical trial: So far, no clinical study has been conducted.
    
    [1] Waelchli, R. ,Bollbuck, B.,Bruns, C., et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorganic & Medicinal Chemistry Letters 16(1), 108-112 (2006).
    [2] Coldewey, S. M.,Rogazzo, M.,Collino, M., et al. Inhibition of I k B kinase reduces the multiple organ dysfunction caused by sepsis in the mouse. Dis.Model Mech. 6, 1031-1042 (2013).
- Properties
  - Alternative Name
    
    IKK Inhibitor VII; [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone, monohydrochloride
    
    CAS Number
    
    1186195-62-9
    
    Molecular Formula
    
    C28H29N5OS·HCl
    
    Molecular Weight
    
    520.1
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤10mg/ml in DMSO;5mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

IKK-16 (hydrochloride)

IKK-16 (hydrochloride)

Background

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