BAY-3827 is a potent and selective AMPK inhibitor with an IC50 of 1.4 nM at low concentrations of ATP (10 µM) and 15 nM at high concentrations of ATP (2 mM). BAY-3827 (0-200 µM) inhibits Aurora A, Flt3, c-Met and Rsk4 with an IC50 of 10 µM ATP. BAY-3827 prevented the phosphorylation of acetyl-CoA carboxylase 1 and showed the strongest antiproliferative activity in androgen-dependent prostate cancer cell lines. BAY-3827 (overnight) strongly reduced the phosphorylation of ACC1 Ser79 in LNCaP and VCaP cells. BAY-3827 (0-200 μM) inhibited Aurora A, Flt3, c-Met and Rsk4, with an IC50 at 10 µM ATP concentration of 1324, 124, 788, and 36 nM, respectively. Phosphorylation of ACC1 Ser79 was reduced to a lesser extent in IMR-32 cells, especially in Colo320 cells. At concentrations less than 10 nM, acting for 6 days, BAY-3827 had a strong inhibitory effect on LNCaP and VCaP cells. At 1 and 5 μM concentrations for 24 and 48 hours, BAY-3827 inhibited the expression of the LIPE gene, reduced AKT3, and blocked the expression of several genes in the CPT family involved in acylcarnitine formation in VCaP cells . At a concentration of 5 μM for 2-4 days, BAY-3827 significantly increased lipid droplet formation, whereas androgen-only treatment did not[1].
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