NIK SMI1

Uses

NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor.

Biological Activity

NIK SMI1 is an orally active, ATP site-targeting, potent and selective NF-KB-inducing kinase inhibitor (h/m NIK IC50 = 230/395 pM; hKHS1/hPKD1/hLRRK2 = 49.6/75.2/247.8 nM) th at selectively disrupts noncanonical NF-KB signaling (anti-LTβR-induced p52 nuclear translocation IC50 = 70 nM; TNFα-induced p65 RelA nuclear translocation IC50 >2 μM). SMI1 inhibits BAFF receptor- and CD40-mediated singling in cultures (human and murine B-cells) and shows in vivo efficacy in the NZB/W F1 murine experimental lupus model (6-400 mg/kg/day, b.i.d. p.o.).