Biochem/physiol Actions
Potent and selective NF-κB-inducing kinase (NIK) inhibitor that selectively disrupts NF-κB activation in cultures and in vivo.
B022 is an ATP site-targeting, potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki = 5 nM against 5 μM ATP using mouse NIK) that inhibits NIK-induced p100-to-p52 processing (IC50 <0.5 μM; Hepa1 cells overexpressing p100 & NIK) and NF-κB2 activity (by 38% by 0.5 μM and 96% by 5 μM B022; HEK293 NIK transfectant with NF-κB reporter plasmid). B022 protects mice from death due to liver-specific NIK overexpression in mice in vivo (30 mg/kg via b.i.d.tail vein injection).