Figure 3.

Cellular efficacy of lead TAK1 inhibitors in THP-1 cells. THP-1 human macrophages were differentiated with PMA (10 ng/mL) for 72 h followed by a rest period in PMA-free media. Cells were pretreated with 10 μM of takinib analogues HS-269, HS-276, and HS-277 followed by LPS (10 ng/mL) stimulation. (a) Relative expression of various cytokines compared to vehicle treatment. (b) TNF, IL-1β, IL-6, GROα, ICAM-1, and CXCL11 expression in naive (N =3 ± SEM), LPS (N =3 ± SEM), and HS-276 (N = 4 ± SEM). (c) HS-276 dose-dependent effects of TNF, IL-6, and IL-1β secretion reported as a percent of vehicle control (DMSO) in THP-1 cells, (n = 3 ± SEM).