biological activity | IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor that acts on IKK-2,IKK complex and IKK-1. IC50 in cell-free test is 40 nM,70 nM and 200 nM respectively. IKK-16 can also inhibit the phosphorylation of LRRK2 Ser935 in cells and the kinase activity of LRRK2 in vitro experiments, with a corresponding IC50 value of 50 nM. |
target | TargetValue IKK2 (Cell-free Assay) 40 nM IKK complex (Cell-free Assay) 70 nM IKK1 (Cell-free Assay) 200 nM |
Target | Value |
IKK2
(Cell-free assay)
| 40 nM |
IKK complex
(Cell-free assay)
| 70 nM |
IKK1
(Cell-free assay)
| 200 nM |
in vitro study | IKK-16 inhibit the expression of TNFα-stimulated adhesion molecule E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 also has the activity of inhibiting IFN γ-induced β2 microglobulin or HLA-DR expression, its titer is 4-10 times lower in these analyses. |
in vivo studies | IKK-16 have oral activity on rats and mice, can inhibit the release of TNF-α induced by lipopolysaccharide in vivo, and can also inhibit neutrophil extravasation in peritonitis induced by thiodal. |
use | [4-[(4-Benzo [B] thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone is a potential novel iκ B kinase 2 (IKK2) inhibitor used in the treatment of various immune/inflammatory disorders. |