N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamidehydrochloride

IKK-16 Hydrochloride is a potential novel IκB kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders.

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 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].

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].

200, 40, and 70 nm for ikkα, ikkβ, and ikk complex, respectively.

Desiccate at -20°C

[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).