bi-605906

Description: BI605906 is a novel and potent IKKbeta inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP. BI605906 inhibits TNFalpha-dependent IkappaB degradation and expression of pro-inflammatory mediators IL-6, IL-1b, and CXCL1/2. In primary hepatocytes from healthy animals, metformin and the IKKbeta (inhibitor of kappa B kinase) inhibitor BI605906 both inhibited tumor necrosis factor-alpha-dependent IkappaB degradation and expression of proinflammatory mediators interleukin-6, interleukin-1beta, and CXCL1/2 (C-X-C motif ligand 1/2). Metformin suppressed IKKalpha/beta activation, an effect that could be separated from some metabolic actions, in that BI605906 did not mimic effects of metformin on lipogenic gene expression, glucose production, and AMP-activated protein kinase activation.

References: Circ Res. 2016 Aug 19; 119(5):652-65.