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].

Signaling Pathways >> Epigenetics >> AMPK

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> AMPK

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]

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]. Cell Proliferation Assay[1] Cell Line: LNCaP, VCaP, 22Rv1, C4-2B, PC-3 and DU-145 prostate cancer cell lines Concentration: 0-10 nM Incubation Time: 6 d Result: Showed strong inhibitory effects for LNCaP and VCaP cells, two prostate cancer cell lines with IC50 values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC50 value of 5.55 nM.

[1]. Lemos C, et al. The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cell Oncol (Dordr). 2021 Jun;44(3):581-594.