IKK-16 (hydrochloride)

A potent inhibitor of IKKs

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库存: 现货

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5mg

￥1225.00

980.00

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10mg

￥2137.00

1710.00

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25mg

￥5450.00

4360.00

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50mg

￥6350.00

5080.00

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货号: ajci8982
CAS: 1186195-62-9
别名: IKK Inhibitor VII
分子式: C28H29N5OS ? HCl
分子量: 520.1
纯度: >98%
溶解度: ≤10mg/ml in DMSO;5mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

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).