Benzamide, N-[5-(3,5-dicyano-1,4-dihydro-1,2,6-trimethyl-4-pyridinyl)-6-fluoro-7-methyl-1H-indazol-3-yl]-2-ethyl-

Uses

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].

Biological Activity

BAY-3827 is a selective and potent inhibitor of AMPK (AMP-activated protein kinase) and RSK1 (ribosomal 6 kinase 1) th at exhibit strong anti-proliferative activity in androgen-dependent prostate cancer cell lines. BAY-3827 strongly down-regulates lipase E (LIPE), cAMP-dependent protein kinase type II-beta regulatory subunit (PRKAR2B), serine-threonine kinase AKT3 and carnitine palmitoyl-transferase 1 (CPT1) family expression levels and impairs lipid flux.

References

[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. DOI:10.1007/s13402-020-00584-8