GSK621 is a specific and potent AMPK activator.

在AML细胞系和初级AML样本中，GSK621显著增强了AMPKα T172位点的磷酸化，这是AMPK激活的标志。在一组20个细胞系中，GSK621抑制了所有20个细胞系的增殖，IC50范围为13-30 μM，并在17个（占85%）细胞系中增加了凋亡。此外，GSK621还触发了自噬，这部分促成了AML细胞的死亡。[1]

在裸鼠体内携带MOLM-14异种移植物的实验中，GSK621（30 mg/kg, i.p.）通过增强AMPK活性和诱导凋亡，有效降低了白血病的生长速度并显著延长了生存期。[1]

AMPK enzymatic assay: HEPG2 cells are treated with increasing doses of A-769662 or GSK621, and ACC S79 phosphorylation is assessed as a surrogate marker for AMPK activation using a commercially available ELISA kit.

Twenty AML cell lines are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo?assay. IC50 of GSK621 among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.(Only for Reference)