IKK 16 hydrochloride ,1186195-62-9

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YZ剂描述：

产品名称：IKK 16 hydrochloride

产品别名：IKK-16 HCl；IKK-16

英文别名：IKK-16 HCl;IKK-16

靶点：IKK2；IKK1；IKK；LRRK2

CAS：1186195-62-9

纯度：>98%

外观：solid

保存方法：Desiccate at -20° C

描述：

IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM. 

溶解性：Soluble in water (50 mM), and DMSO (100 mM).

体外研究：

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.

体内研究：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.

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