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IKK-16(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IKK-16(hydrochloride)图片
CAS NO:1186195-62-9
规格:98%
分子量:520.1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
IκB kinases (IKKs) inhibitor
CAS:1186195-62-9
分子式:C28H29N5OS ? HCl
分子量:520.1
纯度:98%
存储:Store at -20°C

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.


参考文献:
[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).