BAY-3827

• CAT Number: I042676
• CAS Number: 2377576-35-5
• Molecular Formula: C27H25FN6O
• Molecular Weight: 468.53
• Purity: ≥95%
• Synonyms: N-[5-(3,5-dicyano-1,2,6-trimethyl-4H-pyridin-4-yl)-6-fluoro-7-methyl-1H-indazol-3-yl]-2-ethylbenzamide
• InChI: InChI=1S/C27H25FN6O/c1-6-17-9-7-8-10-18(17)27(35)31-26-20-11-19(24(28)14(2)25(20)32-33-26)23-21(12-29)15(3)34(5)16(4)22(23)13-30/h7-11,23H,6H2,1-5H3,(H2,31,32,33,35)
• InChIKey: OZFFKOSQNBBYCA-UHFFFAOYSA-N
• SMILES: CCC1=CC=CC=C1C(=O)NC2=NNC3=C(C(=C(C=C32)C4C(=C(N(C(=C4C#N)C)C)C)C#N)F)C

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].
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].

Reference

[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.
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