GSK621
Application
GSK621 has been used as an AMP-activated kinase ? (AMPK ?) activator to study the antiviral role of AMPK in Zika virus (ZIKV) infection. It has also been used as an AMPK ? activator to study its protective effect on myocardial cells against oxygen-glucose deprivation-re-oxygenation (OGD/R).
Biochem/physiol Actions
GSK621 is a direct AMPK activator that exhibits anti-leukemic (300 µM; MOLM-14, HL-60, OCI-AML3) and anti-glioma (Effec. conc. 10-100 µM; U87MG and U251MG) activity, while displaying little cytotoxicity toward normal hematopoietic progenitors, primary human astrocytes, or HCN-1a neuronal cells. When administered via intraperitoneal injection, GSK621 (30 mg/kg twice daily) is shown to reduce leukemia growth and significantly extend the survival of mice xenografted with MOLM-14 cells. AMPK activation by GSK621 leads to mTOR inhibition and Tetraspanin 8 (Tspan8) downregulation in glioma cells, while GSK621-induced cytotoxicity in acute myeloid leukemia (AML) cells is the result of synthetic lethality, where co-activation of AMPK and mTORC1 activates the eIF2a signaling pathway, which in turn triggers autophagic cell death.
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