BAY-3827

BAY-3827 is a potent and selective AMPK inhibitor with IC₅₀ values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines^[1]. IC50 & Target:IC50: 1.4 nM (AMPK kinase,10 µM ATP), 15 nM (AMPK kinase, 2 mM ATP), 1324 nM (Aurora A), 124 nM (Flt3), 788 nM (c-Met), 36 nM (Rsk4)^[1] In Vitro:BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC₅₀ values of 1.4 nM at low, 10 µM ATP concentration and 15 nM at high, 2 mM ATP concentration^[1].
BAY-3827 (0-200 μM) inhibits Aurora A, Flt3, c-Met and Rsk4 with IC₅₀ values of 1324, 124, 788 and 36 nM , respectively with 10 µM ATP concentration^[1].
BAY-3827 (overnight) strongly reduces ACC1 Ser79 phosphorylation in LNCaP and VCaP cells, and shows a lesser extent in IMR-32 and especially in Colo320 cells^[1].
BAY-3827 (0-10 nM; 6 d) shows strong inhibitory effects to LNCaP and VCaP cells^[1].
BAY-3827 (1 and 5 μM; 24 and 48 h) 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].
BAY-3827 (5 μM; 2-4 d) significantly increases the formation of lipid droplets in comparison to androgen treatment only^[1].