BAY-3827 is a potent and selective AMPK inhibitor with potential antitumor activity, demonstrating antiproliferative effects in an androgen-dependent prostate cancer model and inhibiting the phosphorylation of acetyl CoA carboxylase 1 (ACC-1).

Aurora A:1324 nM, c-Met:788 nM, Rsk4:36 nM, AMPK, 2 mM ATP:15 nM, AMPK,10 µM ATP:1.4 nM, Flt3:124 nM

BAY-3827, in the concentration range of 0-200 μM, inhibits AMPK kinase activity with IC50 values of 1.4 nM at low ATP concentration (10 µM) and 15 nM at high ATP concentration (2 mM)[1].In the concentration range of 0-200 μM, BAY-3827 inhibits Aurora A, Flt3, c-Met, and Rsk4 with IC50 values of 1324, 124, 788, and 36 nM, respectively, at 10 µM ATP concentration[1].After overnight treatment, BAY-3827 strongly reduces ACC1 Ser79 phosphorylation in LNCaP and VCaP cells, with a lesser extent in IMR-32 and especially in Colo320 cells[1].At concentrations of 0-10 nM over 6 days, BAY-3827 exhibits strong inhibitory effects on LNCaP and VCaP cells[1].At concentrations of 1 and 5 μM over 24 and 48 hours, BAY-3827 represses LIPE gene expression, reduces serine/threonine kinase AKT3, and blocks the expression of several genes from the mitochondrial carnitine palmitoyltransferase (CPT) family, which is involved in acyl carnitine formation in VCaP cells[1].
At a concentration of 5 μM over 2-4 days, BAY-3827 significantly increases the formation of lipid droplets compared to androgen treatment only[1].