Uses
IKK-16 is a potential novel IκB kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders.
Definition
ChEBI: [4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone is a N-acylpiperidine and a member of benzamides.
Biological Activity
ikk-16 (ikk inhibitor vii) is a novel inhibitor of iκb kinase (ikk) with the ic50 values of 0.04μm, 0.2μm and 0.07μm for ikk2, ikk1 and ikk complex, respectively [1].ikk-16 (ikk inhibitor vii) is a 2-benzamido-pyrimidines and selective inhibitor of iκb kinase (ikk). ikk-16 has been reported to effectively inhibit tnfα release into plasma upon lps-challenge in the rat. in addition, ikk-16 has been found to be active at thioglycollate-induced peritonitis model in the mouse. furthermore, ikk-16 has revealed to be an orally bio-available in rats and mice, and have significant in vivo activity in an acute model of cytokine release [1].
References
[1] waelchli r1, bollbuck b, bruns c, buhl t, eder j, feifel r, hersperger r, janser p, revesz l, zerwes hg, schlapbach a.design and preparation of 2-benzamido-pyrimidines as inhibitors of ikk. bioorg med chem lett. 2006 jan 1;16(1):108-12. epub 2005 oct 19.
