B022

B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1].

Research Areas >> Inflammation/Immunology

Ki: 4.2 nM (NF-κB-inducing kinase (NIK))[1]

B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1]. B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1]. Western Blot Analysis[1] Cell Line: Hepa1 cells Concentration: 0 μM, 0.5 μM, 5 μM Incubation Time: 12 hours Result: Suppressed NIK-induced p52 formation in a dose-dependent manner. RT-PCR[1] Cell Line: Hepa1 cells Concentration: 0 μM, 0.5 μM, 5 μM Incubation Time: 12 hours Result: Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.

B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses[1]. Animal Model: STOP-NIK male mice (8 weeks) infected with Ad-cre[1] Dosage: 30 mg/kg Administration: Intravenous injection; twice a day; for 10 days Result: Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.

[1]. Ren X, et al. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury. FASEB J. 2017 Feb;31(2):711-718.