Chemical Name: 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Biological ActivityAS 1842856 is a potent and selective Foxo1 inhibitor (IC50 values are 33 nM at Foxo1 and >1 μM at Foxo3a and Foxo4); decreases Foxo-mediated promoter activity by 70%, 20% and 3% at Foxo1, Foxo4 and Foxo3, respectively. Regulates gluconeogenesis both in vitro and in vivo. Attenuates fasting plasma glucose level in diabetic db/db mice. Also suppresses autophagy, adipocyte differentiation and soluble guanylyl cyclase expression. Also inhibits STAT3 signaling in NSCLC. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice.
Nagashima et al.
FoxO1 antagonist suppresses autophagy and lipid droplet growth in adipocytes.
Liu et al.
Cell Cycle, 2016;15:2033
Antagonism of forkhead box subclass O transcription factors elicits loss of soluble guanylyl cyclase expression.
Galley et al.
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