NIK SMI1 is a potent, selective small molecule inhibitor of NF-κB inducing kinase (NIK) with Ki of 230±170 pM; only inhibits 3 out of 222 off-target kinases (KHS1, LRRK2, and PKD1) with >75% inhibition at 1 uM; potently inhibits anti-LTβR-induced nuclear p52 levels in anti-LTβR-stimulated HeLa cells, with no effect on canonical signaling; inhibits BAFF and CD40 signaling, suppresses immune responses in vivo; suppresses disease biomarkers and improves survival and renal function in NZB/W F1 mice.
Cat.No
DC10927
Name
NIK inhibitor 4f(NIK SMI1)
Chemical Properties
CAS
1660114-31-7
Formula
C20H19N3O4
MW
365.38
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
[1]. Blaquiere N, et al. Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase. J Med Chem. 2018 Aug 9;61(15):6801-6813.
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