NIK SMI1 是 NF-Κb 诱导激酶 (NIK) 的选择性抑制剂，能够抑制 NIK 催化的 ATP 水解为 ADP，IC50=0.23±0.17 nM。

NIK SMI1 is an effective and selective NF-κB inducing kinase (NIK) inhibitor. It also inhibits NIK-catalyzed hydrolysis of ATP to ADP (IC50: 0.23±0.17 nM).

NIK SMI1 inhibits the expression of NIK SMI1 response element regulated firefly luciferase reporter gene in HEK293 cells (IC50: 34±6 nM). NIK SMI1 inhibits BAFF-induced B cell (mouse) survival in vitro with an IC50 of 373±64 nM. Consistent with expectations for a NIK inhibitor, NIK SMI1 is shown to inhibit nuclear translocation of p52 (RelB) (IC50=70 nM).

The pharmacology of NIK SMI1 is examined in SD rat, CD-1 mouse, beagle, and cynomologous monkey with 20, 32, 18, and 7.8 mL/kg per min, respectively. The volume of distribution (Vd, L/kg) is 1.35, 1.58, 0.778, and 1.39, respectively. C57BL/6 mice are treated twice daily for 7 days with orally administered NIK SMI1 or with three injections of recombinant BAFF receptor fusion protein (Br3- mIgG2a) over the course of the 7-day experiment as a positive control .

1660114-31-7

C20H19N3O4

365.38

DMSO:100 mg/mL (273.69 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years